Alan Paul Kozikowski

Alan Paul Kozikowski's AcademicInfluence.com Rankings

Chemistry

#2051

World Rank

#2897

Historical Rank

Organic Chemistry

#287

World Rank

#350

Historical Rank

chemistry Degrees

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Chemistry

Alan Paul Kozikowski's Degrees

PhD Chemistry University of California, Berkeley
Bachelors Chemistry Stanford University

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Alan Paul Kozikowski's Published Works

Number of citations in a given year to any of this author's works

Total number of citations to an author for the works they published in a given year. This highlights publication of the most important work(s) by the author

Published Works

Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A. (2010) (591)
The isoxazoline route to the molecules of nature (1984) (461)
HDAC6 inhibitors reverse axonal loss in a mouse model of mutant HSPB1–induced Charcot-Marie-Tooth disease (2011) (400)
Structure of acetylcholinesterase complexed with the nootropic alkaloid, (–)-huperzine A (1997) (338)
Therapeutic effects of PKC activators in Alzheimer's disease transgenic mice. (2004) (309)
Transition Metals in Organic Synthesis (1976) (300)
HDAC6 is a target for protection and regeneration following injury in the nervous system (2009) (277)
Biodistribution, Tumor Detection, and Radiation Dosimetry of 18F-DCFBC, a Low-Molecular-Weight Inhibitor of Prostate-Specific Membrane Antigen, in Patients with Metastatic Prostate Cancer (2012) (271)
Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis. (2009) (256)
A series of halogenated heterodimeric inhibitors of prostate specific membrane antigen (PSMA) as radiolabeled probes for targeting prostate cancer. (2009) (252)
Radiolabeled Small-Molecule Ligands for Prostate-Specific Membrane Antigen: In vivo Imaging in Experimental Models of Prostate Cancer (2005) (242)
The amino terminus of tau inhibits kinesin‐dependent axonal transport: Implications for filament toxicity (2009) (235)
Histone Deacetylase 6 and Heat Shock Protein 90 Control the Functions of Foxp3+ T-Regulatory Cells (2011) (229)
Synthesis and evaluation of technetium-99m- and rhenium-labeled inhibitors of the prostate-specific membrane antigen (PSMA). (2008) (217)
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth. (2000) (216)
N-[N-[(S)-1,3-Dicarboxypropyl]Carbamoyl]-4-[18F]Fluorobenzyl-l-Cysteine, [18F]DCFBC: A New Imaging Probe for Prostate Cancer (2008) (212)
Novel PI analogues selectively block activation of the pro-survival serine/threonine kinase Akt. (2003) (208)
NAAG peptidase inhibitors and their potential for diagnosis and therapy (2005) (204)
Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase). (2001) (190)
Synthesis of urea-based inhibitors as active site probes of glutamate carboxypeptidase II: efficacy as analgesic agents. (2004) (182)
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. (2008) (167)
Epigenetic Regulation of Autophagy by the Methyltransferase G9a (2013) (162)
RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells (2012) (154)
2-Aryl-3-indoleacetamides (FGIN-1): a new class of potent and specific ligands for the mitochondrial DBI receptor (MDR). (1992) (153)
Methods for the stereoselective cis cyanohydroxylation and carboxyhydroxylation of olefins (1983) (138)
Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. (2012) (136)
Interactions between human glutamate carboxypeptidase II and urea-based inhibitors: structural characterization. (2008) (131)
Sazetidine-A, A Novel Ligand That Desensitizes α4β2 Nicotinic Acetylcholine Receptors without Activating Them (2006) (131)
Why Hydroxamates May Not Be the Best Histone Deacetylase Inhibitors—What Some May Have Forgotten or Would Rather Forget? (2016) (129)
Preferential inhibition of Akt and killing of Akt-dependent cancer cells by rationally designed phosphatidylinositol ether lipid analogues. (2004) (129)
Studies in Polyphenol Chemistry and Bioactivity. 1. Preparation of Building Blocks from (+)-Catechin. Procyanidin Formation. Synthesis of the Cancer Cell Growth Inhibitor, 3- O -Galloyl-(2 R ,3 R )-epicatechin-4β,8-[3- O -galloyl-(2 R ,3 R )-epicatechin] (1999) (128)
Specific ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in human colorectal cancer cells (2001) (128)
Indoleamides are active against drug-resistant Mycobacterium tuberculosis (2013) (127)
NAAG peptidase inhibition reduces locomotor activity and some stereotypes in the PCP model of schizophrenia via group II mGluR (2004) (125)
HDAC inhibitor increases histone H3 acetylation and reduces microglia inflammatory response following traumatic brain injury in rats (2008) (120)
Chemistry, Pharmacology, and Clinical Efficacy of the Chinese Nootropic Agent Huperzine A (1999) (117)
A practical synthesis of the Chinese "nootropic" agent huperzine A: a possible lead in the treatment of Alzheimer's disease (1989) (112)
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. (2008) (112)
Indole-2-carboxamide-based MmpL3 Inhibitors Show Exceptional Antitubercular Activity in an Animal Model of Tuberculosis Infection. (2016) (111)
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. (2009) (109)
Divergent roles of histone deacetylase 6 (HDAC6) and histone deacetylase 11 (HDAC11) on the transcriptional regulation of IL10 in antigen presenting cells. (2014) (109)
Chemical origins of isoform selectivity in histone deacetylase inhibitors. (2008) (108)
Histone deacetylase 6 inhibition improves memory and reduces total tau levels in a mouse model of tau deposition (2014) (106)
Targeting histone deacetylase 6 mediates a dual anti‐melanoma effect: Enhanced antitumor immunity and impaired cell proliferation (2015) (105)
Studies in polyphenol chemistry and bioactivity. 4.(1) Synthesis of trimeric, tetrameric, pentameric, and higher oligomeric epicatechin-derived procyanidins having all-4beta,8-interflavan connectivity and their inhibition of cancer cell growth through cell cycle arrest. (2003) (105)
11C-MCG: synthesis, uptake selectivity, and primate PET of a probe for glutamate carboxypeptidase II (NAALADase). (2002) (105)
Functional differences in epigenetic modulators-superiority of mercaptoacetamide-based histone deacetylase inhibitors relative to hydroxamates in cortical neuron neuroprotection studies. (2007) (105)
Molecular Pathways: Revisiting Glycogen Synthase Kinase-3β as a Target for the Treatment of Cancer (2017) (102)
Preliminary structure-activity relationships and biological evaluation of novel antitubercular indolecarboxamide derivatives against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains. (2013) (102)
INOC route to carbocyclics: A formal total synthesis of (±)-sarkomycin (1982) (101)
Highly Potent and Specific GSK‐3β Inhibitors That Block Tau Phosphorylation and Decrease α‐Synuclein Protein Expression in a Cellular Model of Parkinson's Disease (2006) (99)
Selective HDAC6 inhibitors improve anti-PD-1 immune checkpoint blockade therapy by decreasing the anti-inflammatory phenotype of macrophages and down-regulation of immunosuppressive proteins in tumor cells (2019) (98)
Novel Inhibitors of Human Histone Deacetylase (HDAC) Identified by QSAR Modeling of Known Inhibitors, Virtual Screening, and Experimental Validation (2009) (96)
Prediction of the binding sites of huperzine A in acetylcholinesterase by docking studies (1994) (95)
Construction of optically pure tryptophans from serine derived aziridine-2-carboxylates (1989) (94)
NAAG peptidase inhibitor increases dialysate NAAG and reduces glutamate, aspartate and GABA levels in the dorsal hippocampus following fluid percussion injury in the rat (2006) (91)
From serendipity to rational antituberculosis drug discovery of mefloquine-isoxazole carboxylic acid esters. (2009) (91)
Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. (1993) (91)
Diastereofacial Selection in Nitrile Oxide Cycloaddition Reactions. The Anti-Directing Effect of an Allylic Oxygen and Some New Results on the Ring Metalation of Isoxazolines. A Synthesis of (±)-Blastmycinone. (1984) (90)
Antinociceptive effects of N‐acetylaspartylglutamate (NAAG) peptidase inhibitors ZJ‐11, ZJ‐17 and ZJ‐43 in the rat formalin test and in the rat neuropathic pain model (2004) (90)
Peroxisome Proliferator-Activated Receptor δ and γ Agonists Differentially Alter Tumor Differentiation and Progression during Mammary Carcinogenesis (2005) (90)
Identification of a more potent analogue of the naturally occurring alkaloid huperzine A. Predictive molecular modeling of its interaction with AChE (1996) (90)
Design, Synthesis, and SAR Studies of Mefloquine‐Based Ligands as Potential Antituberculosis Agents (2006) (89)
Activated forms of H-RAS and K-RAS differentially regulate membrane association of PI3K, PDK-1, and AKT and the effect of therapeutic kinase inhibitors on cell survival. (2005) (88)
Tubastatin A, an HDAC6 inhibitor, alleviates stroke-induced brain infarction and functional deficits: potential roles of α-tubulin acetylation and FGF-21 up-regulation (2016) (88)
Synthesis of Huperzine A and Its Analogues and Their Anticholinesterase Activity (1991) (85)
Intramolecular nitrile oxide cycloaddition (INOC) reactions in the indole series. 2. Total synthesis of racemic and optically active paliclavine and 5-epi-paliclavine (1981) (84)
Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells. (2012) (84)
A Novel Role for Histone Deacetylase 6 in the Regulation of the Tolerogenic STAT3/IL-10 Pathway in APCs (2014) (82)
An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity. (2013) (81)
Specific inhibition of the Akt1 pleckstrin homology domain by D-3-deoxy-phosphatidyl-myo-inositol analogues. (2003) (81)
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications. (2006) (80)
Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1. (2004) (79)
Stimulation of brain steroidogenesis by 2-aryl-indole-3-acetamide derivatives acting at the mitochondrial diazepam-binding inhibitor receptor complex. (1993) (79)
Antinociceptive Pharmacology of N-(4-Chlorobenzyl)-N′-(4-hydroxy-3-iodo-5-methoxybenzyl) Thiourea, a High-Affinity Competitive Antagonist of the Transient Receptor Potential Vanilloid 1 Receptor (2007) (78)
Structure-based design leads to the identification of lithium mimetics that block mania-like effects in rodents. possible new GSK-3beta therapies for bipolar disorders. (2007) (78)
A palladium-catalyzed route to huperzine A and its analogues and their anticholinesterase activity (1993) (77)
HDAC6 is a therapeutic target in mutant GARS-induced Charcot-Marie-Tooth disease (2018) (76)
A chemical basis for recognition of nonpeptide antigens by human γδ T cells* (2000) (76)
Drug design for neuroscience (1993) (75)
Design, Synthesis, and Pharmacological Evaluation of Mefloquine‐Based Ligands as Novel Antituberculosis Agents (2007) (74)
Palladium catalyzed synthesis of annelated indoles (1991) (74)
Utilization of an in vivo reporter for high throughput identification of branched small molecule regulators of hypoxic adaptation. (2010) (73)
NAAG peptidase inhibitor reduces acute neuronal degeneration and astrocyte damage following lateral fluid percussion TBI in rats. (2005) (73)
Conversion of Alcohols to Protected Guanidines Using the Mitsunobu Protocol (1994) (73)
Antimalarial Activity of Phenylthiazolyl-Bearing Hydroxamate-Based Histone Deacetylase Inhibitors (2008) (73)
Novel Diketopiperazine Enhances Motor and Cognitive Recovery after Traumatic Brain Injury in Rats and Shows Neuroprotection In Vitro and In Vivo (2003) (72)
Methods for the conversion of isoxazolines to β-hydroxy ketones (1982) (72)
Efficient synthetic routes to fluorinated isosteres of inositol and their effects on cellular growth (1990) (71)
Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them. (2006) (71)
Chemistry of baker's yeast reduction products: Use of optically active (S)-(+)-1-(p-toluenesulfonyl)propan-2-ol and (S)-(+)-1-(phenylsulfonyl)propan-2-ol in synthesis. (1986) (69)
Rational Design and Simple Chemistry Yield a Superior , Neuroprotective HDAC 6 Inhibitor , Tubastatin A (2010) (68)
Studies in polyphenol chemistry and bioactivity. 2. Establishment of interflavan linkage regio- and stereochemistry by oxidative degradation of an O-alkylated derivative of procyanidin B2 to (R)-(-)-2,4-diphenylbutyric acid. (2000) (67)
Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. (2000) (66)
A route to optically pure (-)-huperzine A : molecular modeling and in vitro pharmacology (1991) (65)
A microenvironment-mediated c-Myc/miR-548m/HDAC6 amplification loop in non-Hodgkin B cell lymphomas. (2013) (65)
In pursuit of natural product leads: synthesis and biological evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazole-4-carboxylic acid (A-33853) and its analogues: discovery of N-(2-benzoxazol-2-ylphenyl)benzamides as novel antileishmanial chemotypes. (2008) (65)
Diastereoselection in Intermolecular Nitrile Oxide Cycloaddition (NOC) Reactions: Confirmation of the "Anti-Periplanar Effect" through a Simple Synthesis of 2-Deoxy-d-ribose†. (1982) (64)
Dimethylaluminum methylselenolate: a remarkable reagent for the preparation of active acyl-transfer agents (1978) (64)
A synthetic approach to the cis-fused marine pyranopyrans, (3E)- and (3Z)-dactomelyne. X-ray structure of a rare organomercurial (1990) (63)
Synthesis of the first optically pure, fluorinated inositol 1,4,5-trisphosphate of myo-inositol stereochemistry and its effect on Ca2+ release in Swiss 3T3 cells (1990) (63)
Intramolecular nitrile oxide cycloaddition route to carbocyclics: a formal total synthesis of PGF2α (1984) (62)
Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity. (1997) (62)
Copper(I) promoted acylation reactions. A transition metal mediated version of the Friedel-Crafts reaction [15] (1980) (60)
Evodiamine functions as an agonist for the vanilloid receptor TRPV1. (2004) (60)
A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. (2003) (60)
An improved method for the synthesis of anomerically allylated C-glycopyranosides and C-glycofuranosides. (1982) (59)
Discovery of isoxazole analogues of sazetidine-A as selective α4β2-nicotinic acetylcholine receptor partial agonists for the treatment of depression. (2011) (59)
Phosphatidylinositol Ether Lipid Analogues That Inhibit AKT Also Independently Activate the Stress Kinase, p38α, through MKK3/6-independent and -dependent Mechanisms* (2007) (59)
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. (2010) (59)
Potencies and stereoselectivities of enantiomers of huperzine A for inhibition of rat cortical acetylcholinesterase. (1991) (58)
Comparison of the effects of natural and synthetic huperzine-A on rat brain cholinergic function in vitro and in vivo. (1994) (58)
Histone/protein deacetylase 11 targeting promotes Foxp3+ Treg function (2017) (58)
Enhanced binding of metabotropic glutamate receptor type 5 (mGluR5) PET tracers in the brain of parkinsonian primates (2008) (57)
Participation of mitochondrial diazepam binding inhibitor receptors in the anticonflict, antineophobic and anticonvulsant action of 2-aryl-3-indoleacetamide and imidazopyridine derivatives. (1993) (57)
Peroxisome proliferator-activated receptor delta and gamma agonists differentially alter tumor differentiation and progression during mammary carcinogenesis. (2005) (57)
Pyrido[1,2‐a]benzimidazole‐Based Agents Active Against Tuberculosis (TB), Multidrug‐Resistant (MDR) TB and Extensively Drug‐Resistant (XDR) TB (2011) (56)
Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the tropane skeleton. (1998) (56)
Essential role of HDAC6 in the regulation of PD‐L1 in melanoma (2016) (56)
Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents. (2006) (56)
Total Syntheses of (+)-Himbacine and (+)-Himbeline (1995) (55)
Phencyclidine and Dizocilpine Induced Behaviors Reduced by N-acetylaspartylglutamate Peptidase Inhibition via Metabotropic Glutamate Receptors (2008) (55)
Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies. (2000) (55)
GSK-3 inhibition overcomes chemoresistance in human breast cancer. (2016) (54)
Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development. (2010) (54)
Targeting Mycolic Acid Transport by Indole-2-carboxamides for the Treatment of Mycobacterium abscessus Infections. (2017) (54)
Synthesis and biology of a 7-nitro-2,1,3-benzoxadiazol-4-yl derivative of 2-phenylindole-3-acetamide: a fluorescent probe for the peripheral-type benzodiazepine receptor. (1997) (54)
Molecular modeling studies of the Akt PH domain and its interaction with phosphoinositides. (2001) (54)
A nitrile oxide based entry to 2,3-dihydropyran-4-ones: synthesis of a protected version of compactin lactonë in racemic and optically active forms (1985) (54)
Local administration of N‐acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in peripheral pain in rats (2007) (53)
Cocaine and dopamine differentially protect [3H]mazindol binding sites from alkylation by N-ethylmaleimide. (1992) (53)
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist. (1998) (53)
Searching for new cures for tuberculosis: design, synthesis, and biological evaluation of 2-methylbenzothiazoles. (2009) (53)
Putting the 'HAT' back on survival signalling: the promises and challenges of HDAC inhibition in the treatment of neurological conditions. (2009) (53)
A selective histone deacetylase-6 inhibitor improves BDNF trafficking in hippocampal neurons from Mecp2 knockout mice: implications for Rett syndrome (2014) (52)
Novel TRH analog improves motor and cognitive recovery after traumatic brain injury in rodents. (1999) (51)
Intracerebroventricular administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in inflammatory pain (2008) (51)
Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors. (2005) (51)
Bicyclic-Capped Histone Deacetylase 6 Inhibitors with Improved Activity in a Model of Axonal Charcot-Marie-Tooth Disease. (2016) (51)
Synthesis and biological studies of simplified analogues of lyngbyatoxin A: Use of an isoxazoline-based indole synthesis. Quest for protein kinase C modulators (1989) (50)
Dissociation between duration of action in the forced swim test in mice and nicotinic acetylcholine receptor occupancy with sazetidine, varenicline, and 5-I-A85380 (2011) (50)
Synthesis of 1D-3-deoxy-, 1D-2,3-dideoxy-, and 1D-2,3,6-trideoxy-myo-inositol 1,4,5-trisphosphate from quebrachitol, their binding affinities, and calcium release activity (1993) (50)
Trans-azetidine-2,4-dicarboxylic acid activates neuronal metabotropic receptors. (1993) (49)
Phosphatidylinositol ether lipid analogues induce AMP-activated protein kinase-dependent death in LKB1-mutant non small cell lung cancer cells. (2008) (49)
Inhibition of GSK-3 Induces Differentiation and Impaired Glucose Metabolism in Renal Cancer (2013) (49)
Studies in polyphenol chemistry and bioactivity. 3.(1,2) stereocontrolled synthesis of epicatechin-4alpha,8-epicatechin, an unnatural isomer of the B-type procyanidins. (2001) (48)
Spectrum of activity and molecular correlates of response to phosphatidylinositol ether lipid analogues, novel lipid-based inhibitors of Akt (2006) (48)
Identification and development of novel inhibitors of Toxoplasma gondii enoyl reductase. (2010) (47)
New synthesis and some selected reactions of the potential ergot alkaloid precursor indole-4-carboxaldehyde (1980) (47)
Recognition of Benztropine by the Dopamine Transporter (DAT) Differs from That of the Classical Dopamine Uptake Inhibitors Cocaine, Methylphenidate, and Mazindol as a Function of a DAT Transmembrane 1 Aspartic Acid Residue (2005) (46)
Methoxylation of cocaine reduces binding affinity and produces compounds of differential binding and dopamine uptake inhibitory activity: discovery of a weak cocaine "antagonist". (1993) (46)
Total synthesis of pseudomonic acid C: application of the alkoxyselenation reaction in organic synthesis (1980) (46)
Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. (2009) (45)
Neuroprotective and Nootropic Actions of a Novel Cyclized Dipeptide after Controlled Cortical Impact Injury in Mice (2003) (45)
The isoxazoline route to the hypocholesterolemic agent compactin: use of the isoxazoline as a 1,3-diene equivalent (1987) (45)
Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity. (2000) (45)
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. (2006) (45)
Chemistry, Biology, and QSAR Studies of Substituted Biaryl Hydroxamates and Mercaptoacetamides as HDAC Inhibitors—Nanomolar‐Potency Inhibitors of Pancreatic Cancer Cell Growth (2008) (44)
Identification of amino acid residues involved in the binding of Huperzine A to cholinesterases (1994) (44)
Identification, synthesis, and pharmacological evaluation of tetrahydroindazole based ligands as novel antituberculosis agents. (2010) (43)
A chemical basis for selective recognition of nonpeptide antigens by human delta T cells. (2000) (43)
Delineating the pharmacophoric elements of huperzine A: importance of the unsaturated three-carbon bridge to its AChE inhibitory activity. (1991) (43)
New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha. (2003) (43)
3-Deoxy-D-myo-inositol 1-phosphate, 1-phosphonate, and ether lipid analogues as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth. (1998) (43)
Methoxyphenylethynyl, methoxypyridylethynyl and phenylethynyl derivatives of pyridine: synthesis, radiolabeling and evaluation of new PET ligands for metabotropic glutamate subtype 5 receptors. (2005) (43)
Studies of Benzamide‐ and Thiol‐Based Histone Deacetylase Inhibitors in Models of Oxidative‐Stress‐Induced Neuronal Death: Identification of Some HDAC3‐Selective Inhibitors (2009) (43)
Applications of Organosulfur Chemistry to Organic Synthesis: Total Synthesis of (+)-Himbeline and (+)-Himbacine (1997) (43)
Synthesis, biological evaluation, and structure-activity relationships for 5-[(E)-2-arylethenyl]-3-isoxazolecarboxylic acid alkyl ester derivatives as valuable antitubercular chemotypes. (2009) (42)
Searching for Disease Modifiers—PKC Activation and HDAC Inhibition—A Dual Drug Approach to Alzheimer's Disease that Decreases Aβ Production while Blocking Oxidative Stress (2009) (42)
Synthesis of streptazolin: use of the aza-Ferrier reaction in conjunction with the INOC process to deliver a unique but sensitive natural product (1990) (42)
Novel HDAC Inhibitors with Radiosensitizing Properties (2005) (42)
The RAD51-stimulatory compound RS-1 can exploit the RAD51 overexpression that exists in cancer cells and tumors. (2014) (42)
Dimethylaluminum methaneselenolate—a useful reagent for the preparation of selenoesters. A new friedel-crafts acylation procedure promoted by Cu(I) (1985) (41)
Synthesis and biological activity of novel neuroprotective diketopiperazines. (2002) (41)
Prediction of the binding site of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine in acetylcholinesterase by docking studies with the SYSDOC program (1994) (40)
Ring opening reactions of aziridines with organometallics (1979) (40)
Dysregulation of glutamate carboxypeptidase II in psychiatric disease (2008) (40)
Design and Synthesis of Aryl Ether Inhibitors of the Bacillus Anthracis Enoyl‐ACP Reductase (2008) (40)
Growth factor and oncogene signalling pathways as targets for rational anticancer drug development. (1991) (40)
Identification of novel α4β2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity. (2012) (40)
Discovery of a New Isoxazole-3-hydroxamate Based Histone Deacetylase 6 Inhibitor SS-208 with Anti-tumor Activity in Syngeneic Melanoma Mouse Models. (2019) (39)
Synthesis and evaluation of a photolyzable derivative of sphingosine 1-phosphate--caged SPP. (1998) (39)
Structure-activity relationships of compounds targeting mycobacterium tuberculosis 1-deoxy-D-xylulose 5-phosphate synthase. (2008) (39)
Protection of alcohols as their (p-methoxybenzyloxy)methyl ethers. (1988) (39)
Phosphoniosilylation: an efficient and practical method for the β-functionalization of enones (1986) (39)
Recent Developments Using Small Molecules to Target RAD51: How to Best Modulate RAD51 for Anticancer Therapy? (2016) (39)
Cellular sensitization to cis-diamminedichloroplatinum(II) by novel analogues of the protein kinase C activator lyngbyatoxin A. (1991) (38)
Metabotropic glutamate receptor subtypes differentially influence neuronal recovery from in vitro hypoxia/hypoglycemia in rat hippocampal slices (1995) (38)
A patent review of histone deacetylase 6 inhibitors in neurodegenerative diseases (2014-2019) (2019) (38)
Intramolecular [3 + 2] cycloaddition reactions in the indole series "the nitrile oxide route to the ergot alkaloids". 1. Chanoclavine I [9] (1980) (38)
Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors. (2001) (38)
Chemistry and Pharmacology of Nicotinic Ligands Based on 6‐[5‐(Azetidin‐2‐ylmethoxy)pyridin‐3‐yl]hex‐5‐yn‐1‐ol (AMOP‐H‐OH) for Possible Use in Depression (2009) (38)
Total synthesis of the unique mycotoxin α-cyclopiazonic acid (αCA): An unusual dimethylzinc-mediated replacement of a phenylthio substituent by a methyl group and a contrathermodynamic Raney nickel desulfurization reaction (1984) (38)
Isoxazolyl-serine-based agonists of peroxisome proliferator-activated receptor: design, synthesis, and effects on cardiomyocyte differentiation. (2004) (38)
Recent Developments in Novel Antidepressants Targeting α4β2-Nicotinic Acetylcholine Receptors (2014) (38)
π-Facial selection in intermolecular Diels-Alder reactions: total syntheses of (+)-actinobolin and (+)-5, 6, 10-triepi-actinobolin. (1987) (37)
Synthesis of Novel Four-Membered Ring Amino Acids as Modulators of the N-Methyl-D-Aspartate(NMDA) Receptor Complex (1991) (37)
Total synthesis of the C-nucleoside dl-showdomycin by a Diels-Alder, retrograde Dieckmann strategy (1981) (37)
5-HT2C Agonists Modulate Schizophrenia-Like Behaviors in Mice (2017) (36)
The intramolecular nitrile oxide cycloaddition (INOC) route to the ergot alkaloids: Use of the isoxazoline to γ-amino alcohol conversion in the total synthesis of (+)-paliclavine (1984) (36)
Design and Synthesis of a PSMA Inhibitor–Doxorubicin Conjugate for Targeted Prostate Cancer Therapy (2006) (36)
Molecular modeling of the interactions of glutamate carboxypeptidase II with its potent NAAG-based inhibitors. (2002) (36)
Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. (2005) (36)
Chemistry and biology of the 2β-alkyl-3β-phenyl analogues of cocaine : subnanomolar affinity ligands that suggest a new pharmacophore model at the C-2 position (1995) (36)
Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population. (2004) (35)
Brain Penetrable Histone Deacetylase 6 Inhibitor SW-100 Ameliorates Memory and Learning Impairments in a Mouse Model of Fragile X Syndrome. (2018) (35)
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3. (2004) (35)
Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. (1992) (35)
Identification of a Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitor, BIP-135, that Prolongs the Median Survival Time of Δ7 SMA KO Mouse Model of Spinal Muscular Atrophy. (2012) (34)
Effect of alteration of the heterocyclic nucleus of ILV on its isoform selectivity for PKC. Palladium catalyzed route to benzofuran analogues of ILV (1995) (34)
Bis(dimethylaluminum) 1,3-propanedithiolate–a useful reagent in the conversion of esters to unsaturated aldehydes and ketones (1975) (33)
Classification and Allosteric Modulation of Excitatory Amino Acid Signal Transduction in Brain Slices and Primary Cultures of Cerebellar Neurons (1988) (33)
Chemistry and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile. (2012) (33)
Design and synthesis of 2-pyridones as novel inhibitors of the Bacillus anthracis enoyl-ACP reductase. (2008) (33)
Development of Small Molecules that Specifically Inhibit the D-loop Activity of RAD51. (2016) (33)
Synthesis and bioactivity of a new class of rigid glutamate analogues. Modulators of the N-methyl-D-aspartate receptor. (1990) (33)
Thiol-Based Potent and Selective HDAC6 Inhibitors Promote Tubulin Acetylation and T-Regulatory Cell Suppressive Function. (2015) (32)
Reinforcing Strength of a Novel Dopamine Transporter Ligand: Pharmacodynamic and Pharmacokinetic Mechanisms (2002) (32)
A simplified route to the phosphatidylinositol cascade inhibitor --- (-)-1L-1-deoxy-1-fluoro-Myo-inositol (1989) (32)
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity. (2009) (32)
Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine. (1992) (31)
Active benzimidazole derivatives targeting the MmpL3 transporter in Mycobacterium abscessus. (2019) (31)
Identification of a Glycogen Synthase Kinase‐3β Inhibitor that Attenuates Hyperactivity in CLOCK Mutant Mice (2011) (31)
Characterization of maleimide-based glycogen synthase kinase-3 (GSK-3) inhibitors as stimulators of steroidogenesis. (2013) (31)
Novel N-Benzoyl-2-Hydroxybenzamide Disrupts Unique Parasite Secretory Pathway (2012) (30)
Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer (2019) (30)
The nitrile oxide cycloaddition (NOC) route to a multipurpose C-nucleoside intermediate: A new class of C-nucleosides [6] (1983) (30)
Glutamate carboxypeptidase II levels in rodent brain using [125I]DCIT quantitative autoradiography (2005) (30)
Putting the ‘HAT’ back on survival signalling: the promises and challenges of HDAC inhibition in the treatment of neurological conditions (2009) (30)
HDAC6 inhibition promotes α-tubulin acetylation and ameliorates CMT2A peripheral neuropathy in mice (2020) (30)
Organic reactions at high pressure. Cycloadditions of enamines and dienamines [17] (1974) (30)
Glycogen Synthase Kinase-3 Inhibition Sensitizes Pancreatic Cancer Cells to Chemotherapy by Abrogating the TopBP1/ATR-Mediated DNA Damage Response (2019) (30)
Synthesis of structural analogues of lyngbyatoxin A and their evaluation as activators of protein kinase C. (1991) (30)
Synthesis, biological evaluation, and structure-activity relationships of N-benzoyl-2-hydroxybenzamides as agents active against P. falciparum (K1 strain), Trypanosomes, and Leishmania. (2012) (29)
CoMFA study of piperidine analogues of cocaine at the dopamine transporter: exploring the binding mode of the 3 alpha-substituent of the piperidine ring using pharmacophore-based flexible alignment. (2004) (29)
Dipolar Cycloaddition Route to Diverse Analogues of Cocaine: The 6- and 7-Substituted 3-Phenyltropanes. (1997) (29)
NOC approach to spiroketals: a total synthesis of (±)-talaromycin B (1984) (29)
GSK-3β Governs Inflammation-Induced NFATc2 Signaling Hubs to Promote Pancreatic Cancer Progression (2016) (29)
3-hydroxy-2-pyrone as a vinylketene equivalent for the synthesis of dihydrophenols and cyclohexenones (1975) (29)
Synthesis and metabotropic receptor activity of the novel rigidified glutamate analogues (+)- and (-)-trans-azetidine-2,4-dicarboxylic acid and their N-methyl derivatives. (1993) (29)
A synthesis of 3-substituted pyrroles through the halogen-metal exchange reaction of 3-bromo-1-(triisopropylsilyl)pyrrole (1984) (29)
Role of the increased noradrenergic neurotransmission in drug self-administration. (2006) (29)
Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. (2020) (29)
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity. (2003) (28)
Structural basis of RasGRP binding to high-affinity PKC ligands. (2002) (28)
Chiral Mercaptoacetamides Display Enantioselective Inhibition of Histone Deacetylase 6 and Exhibit Neuroprotection in Cortical Neuron Models of Oxidative Stress (2012) (28)
Total synthesis of streptazolin - an application of the aza-analogue of the ferrier rearrangement (1985) (28)
A simplified route to a key intermediate in the synthesis of the Chinese nootropic agent huperzine A (1990) (28)
A model study for the synthesis of the hexahydrobenzofuran fragment of the milbemycins and avermectins. (1986) (28)
Methods for Pyranoannulation: An Approach to a New Class of Polyethers. (1985) (28)
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth. (2001) (28)
Combination Treatment with the GSK-3 Inhibitor 9-ING-41 and CCNU Cures Orthotopic Chemoresistant Glioblastoma in Patient-Derived Xenograft Models12 (2017) (28)
The Novel Triple Reuptake Inhibitor JZAD-IV-22 Exhibits an Antidepressant Pharmacological Profile without Locomotor Stimulant or Sensitization Properties (2010) (27)
Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II. (2012) (27)
Synthesis of 2-substituted δ3-Piperidines: The nitrogen analogue of the Ferrier rearrangement. An approach to streptazolin (1984) (27)
Hydroxymercuration-reductive coupling route to .delta.-lactones. Synthesis of malyngolide, an antibiotic from a marine blue-green alga (1982) (27)
Synthesis, molecular modeling, 2-D NMR, and biological evaluation of ILV mimics as potential modulators of protein kinase C (1993) (27)
Metabotropic glutamate receptor agonist trans-azetidine-2,4-dicarboxylic acid facilitates maintenance of LTP in the dentate gyrus in vivo (1995) (27)
Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors. (2000) (27)
The combination of huperzine A and imidazenil is an effective strategy to prevent diisopropyl fluorophosphate toxicity in mice (2008) (27)
TUNING THE SELECTIVITY OF MONOAMINE TRANSPORTER INHIBITORS BY THE STEREOCHEMISTRY OF THE NITROGEN LONE PAIR (1998) (27)
STRUCTURE-BASED DESIGN OF A NEW CLASS OF PROTEIN KINASE C MODULATORS (1998) (27)
Molecular recognition at the myo-inositol 1,4,5-trisphosphate receptor. 3-position substituted myo-inositol 1,4,5-trisphosphate analogues reveal the binding and Ca2+ release requirements for high affinity interaction with the myo-inositol 1,4,5-trisphosphate receptor. (1994) (27)
Insights into the structural determinants required for high-affinity binding of chiral cyclopropane-containing ligands to α4β2-nicotinic acetylcholine receptors: an integrated approach to behaviorally active nicotinic ligands. (2012) (26)
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. (2015) (26)
Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivity (1995) (26)
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization. (2004) (26)
Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects. (2000) (25)
Synthesis and protein kinase C binding activity of benzolactam-V7. (1999) (25)
Organometallic compounds in organic synthesis: nucleophilic substitution reactions of N-methylindoletricarbonyl chromium(0) (1978) (25)
Total synthesis of the clavicipitic acids by an intramolecular azide cycloaddition strategy (1984) (25)
A key intermediate for the synthesis of maytansine and related antitumor agents (1978) (25)
Author Correction: Selective HDAC6 inhibitors improve anti-PD-1 immune checkpoint blockade therapy by decreasing the anti-inflammatory phenotype of macrophages and down-regulation of immunosuppressive proteins in tumor cells (2019) (25)
The Isoxazoline Route to α-Methylene Lactones. (1983) (25)
Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites. (2003) (25)
D-3-Deoxy-3-substitutedmyo-inositol analogues as inhibitors of cell growth (1991) (25)
Synthesis and Pharmacological Evaluation of 8‐ and 9‐Substituted Benzolactam‐V8 Derivatives as Potent Ligands for Protein Kinase C, a Therapeutic Target for Alzheimer's Disease (2006) (25)
Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors. (2017) (24)
Design and Discovery of Functionally Selective Serotonin 2C (5-HT2C) Receptor Agonists. (2016) (24)
Synthetic studies in the indole series. Preparation of the unique antibiotic alkaloid chuangxinmycin by a nitro group displacement reaction (1982) (24)
Synthesis, molecular modeling, and biology of the 1-benzyl derivative of APDC-AN apparent mGluR6 selective ligand (1997) (24)
Synthesis and anticholinesterase activity of huperzine A analogues containing phenol and catechol replacements for the pyridone ring. (1998) (24)
Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring. (2004) (23)
Benzolactam (BL) enhances sAPP secretion in fibroblasts and in PC12 cells. (1999) (23)
A convenient method for the synthesis of unsymmetrical 3,4-disubstituted pyrroles (1990) (23)
Probing ergot alkaloid biosynthesis: Synthesis and feeding of a proposed intermediate along the biosynthetic pathway. A new amidomalonate for tryptophan elaboration (1988) (23)
Anti-gal antibodies in humans and 1, 3α-galactosyltransferase knock-out mice (2000) (23)
Synthesis and biology of the rigidified glutamate analogue, trans-2-carboxyazetidine-3-acetic acid (t-CAA) (1996) (23)
HTS and Rational Drug Design to Generate a Class of 5‐HT2C‐Selective Ligands for Possible Use in Schizophrenia. (2010) (23)
Structure-activity relationship studies of N-sulfonyl analogs of cocaine: role of ionic interaction in cocaine binding. (1994) (23)
Chemical Medicine: Novel 10‐Substituted Cytisine Derivatives with Increased Selectivity for α4β2 Nicotinic Acetylcholine Receptors (2007) (23)
Ketene Thioacetal Route to γ-Lactones. Effect of Carbonyl Hardness on Reaction-Site Selectivity and a Unique Preparation of 3-Methyl-5-phenyl-2(5H)-furanone (1980) (23)
Identification of HDAC6‐Selective Inhibitors of Low Cancer Cell Cytotoxicity (2016) (23)
Lewis acid assisted condensations between a 5-methoxyisoxazolidine and silicon-based nucleophiles: γ-amino alcohol building block in the synthesis of agroclavine I (1985) (23)
Inositol Analogs as Potential Anticancer Therapeutics (1994) (23)
Synthesis of 7-substituted benzolactam-V8s and their selectivity for protein kinase C isozymes. (2002) (23)
Why Academic Drug Discovery Makes Sense (2006) (22)
A facile synthesis of substituted conjugated cyclohexadienes. (1973) (22)
Synthesis of fluorine-containing isosteres of sphingosine as inactivators of protein kinase C (1990) (22)
Probing the topography of kainate recognition sites: Synthesis of a novel oxetane containing kainic acid analogue. (1990) (22)
Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. (1999) (22)
Biological Evaluation of Potent Triclosan‐Derived Inhibitors of the Enoyl–Acyl Carrier Protein Reductase InhA in Drug‐Sensitive and Drug‐Resistant Strains of Mycobacterium tuberculosis (2014) (22)
Synthesis and biology of 1D-3-deoxyphosphatidylinositol: a putative antimetabolite of phosphatidylinositol-3-phosphate and an inhibitor of cancer cell colony formation. (1995) (22)
Synthesis of the thiazolone analogue of the acetylcholinesterase inhibitor, huperzine A (1994) (22)
Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters. (1998) (22)
1,3-Diethoxycarbonylallene: an active dienophile and ethoxycarbonylketen equivalent in the synthesis of antibiotic C-nucleosides (1977) (22)
An Approach to Open Chain and Modified Heterocyclic Analogues of the Acetylcholine-sterase Inhibitor, Huperzine A, through a Bicyclo[3.3.1]nonane Intermediate (1994) (22)
An improved synthetic route to huperzine A; new analogues and their inhibition of acetylcholinesterase (1993) (21)
Pharmacological and behavioral analysis of the effects of some bivalent ligand-based monoamine reuptake inhibitors. (2001) (21)
General and Stereospecific Route to 9-Substituted, 8,9-Disubstituted, and 9,10-Disubstituted Analogues of Benzolactam-V8 (1999) (21)
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. (2003) (21)
Ketamine and N-acetylaspartylglutamate peptidase inhibitor exert analgesia in bone cancer pain. (2006) (21)
11C-MCG: Synthesis, Uptake Selectivity, and Primate PET of a Probe for Glutamate Carboxypeptidase II (NAALADase) (2002) (21)
Application of the bivalent ligand approach to the design of novel dimeric serotonin reuptake inhibitors [4] (2000) (21)
An examination of the extent of diasterofacial selection in the reactions of a chiral nitrile oxide with achiral alkenes: a route to β-hydroxy carboxylic acids (1983) (21)
Synthesis and biological evaluation of (±)-Z-huperzine A (1990) (20)
Natural product leads for drug discovery: isolation, synthesis and biological evaluation of 6-cyano-5-methoxyindolo[2,3-a]carbazole based ligands as antibacterial agents. (2009) (20)
Studies in Polyphenol Chemistry and Bioactivity. Part 1. Preparation of Building Blocks from (+)-Catechin. Procyanidin Formation. Synthesis of the Cancer Cell Growth Inhibitor, 3-O-Galloyl-(2R,3R)-epicatechin-4β,8- [3-O-galloyl-(2R,3R)-epicatechin]. (2000) (20)
Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (Sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) as α4β2-nicotinic acetylcholine receptor-selective partial agonists. (2010) (20)
A Tandem Michael Addition Ring-Closure Route to the Metabotropic Receptor Ligand α-(Hydroxymethyl)glutamic Acid and Its γ-Alkylated Derivatives (2001) (20)
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. (2016) (20)
A useful approach to tricyclic compounds and medium ring diketones through the phosphoniosilylation reaction. (1986) (20)
Diastereoface selection in the inoc reaction (1982) (20)
Modification of Triclosan Scaffold in Search of Improved Inhibitors for Enoyl‐Acyl Carrier Protein (ACP) Reductase in Toxoplasma gondii (2013) (20)
Oxazoles in organic chemistry. Synthesis of the antitumor agent ellipticine. (1977) (20)
An efficacious synthesis of aryl and heteroaryl C-glycosides (1987) (20)
Advances with phospholipid signalling as a target for anticancer drug development. (1995) (20)
Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors. (2001) (19)
Synthesis of 5-endo-, 5-exo-, 6-endo- and 6-exo-hydroxylated analogues of epibatidine (2003) (19)
Synthesis of (±)-10,10-dimethylhuperzine A — a huperzine analogue possessing a slower enzyme off-rate (1996) (19)
Structural requirements of lyngbyatoxin A for activation and downregulation of protein kinase C. (1992) (19)
Creating zinc monkey wrenches in the treatment of epigenetic disorders. (2009) (19)
Synthesis and Biological Activity of D-3-Deoxy-3-Fluorophosphatidylinositol—A New Direction in the Design of non-DNA Targeted Anticancer Agents† (1992) (19)
Synthesis of the benzenoid analogue of the Chinese nootropic agent huperzine A (1989) (19)
Synthesis of a hybrid analog of the acetylcholinesterase inhibitors huperzine A and huperzine B (2001) (18)
HTS, Chemical Hybridization, and Drug Design Identify a Chemically Unique Antituberculosis Agent–Coupling Serendipity and Rational Approaches to Drug Discovery (2007) (18)
Rational Design of Suprastat, a Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models. (2020) (18)
Controlling Extra- and Intramacrophagic Mycobacterium abscessus by Targeting Mycolic Acid Transport (2017) (18)
Ceramide mediates nanovesicle shedding and cell death in response to phosphatidylinositol ether lipid analogs and perifosine (2012) (18)
We Need 2C but Not 2B: Developing Serotonin 2C (5‐HT2C) Receptor Agonists for the Treatment of CNS Disorders (2015) (18)
Huperzine A--a potent acetylcholinesterase inhibitor of use in the treatment of Alzheimer's disease. (1991) (18)
The synthesis of tricyclic cocaine analogs via the 1,3-dipolar cycloaddition of oxidopyridinium betaines (1998) (18)
Regional Anesthesia and Pain (2006) (18)
Synthesis of optically active thiadecalins and thiahydrindans by a proline-catalyzed intramolecular Michael reaction (1989) (18)
3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth. (2001) (18)
A NOVEL POTASSIUM HYDRIDE INDUCED REORGANIZATION REACTION. SYNTHESIS OF CONDENSED HETEROCYCLES (1978) (18)
Derivatives of 3-isoxazolecarboxylic acid esters: a potent and selective compound class against replicating and nonreplicating Mycobacterium tuberculosis. (2012) (18)
Synthesis and pharmacological evaluation of benzofuran-acetamides as "antineophobic" mitochondrial DBI receptor complex ligands. (1998) (18)
Oxazoles in organic chemistry. 2. Application to the synthesis of benzylisoquinoline alkaloids (1980) (17)
Molecular modeling, structure--activity relationships and functional antagonism studies of 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketones as a novel class of dopamine transporter inhibitors. (2001) (17)
Anti-Gal antibodies in humans and 1, 3alpha-galactosyltransferase knock-out mice. (2000) (17)
Complete 1H NMR spectral fingerprint of huperzine A (2007) (17)
18F-ZW-104: A New Radioligand for Imaging Neuronal Nicotinic Acetylcholine Receptors—In Vitro Binding Properties and PET Studies in Baboons (2009) (17)
Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models. (2017) (17)
A model study for the synthesis of the tumor promoting agents lyngbyatoxin a and teleocidin b—further aspects of a new isoxazoline-based indole synthesis. (1985) (17)
Synthesis of D-3-deoxy-myo-inositol 1,4,5-trisphosphate and its effect on Ca2+ release in NIH 3T3 cells (1990) (17)
Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor. (2018) (17)
Mutation of Rv2887, a marR-Like Gene, Confers Mycobacterium tuberculosis Resistance to an Imidazopyridine-Based Agent (2015) (17)
Synthesis of erythro-ω-aminosphingosine and preparation of an affinity column for sphingosine kinase purification (1996) (17)
[(4 + 2) + (3 + 2)] Route to multiply fused ring systems: A new notion in polycycle construction (1984) (17)
An approach to modified heterocyclic analogues of huperzine A and isohuperzine A. Synthesis of the pyrimidone and pyrazole analogues, and their anticholinesterase activity (1996) (17)
A useful method for converting 2° alcohols to their chlorides with retention of configuration (1988) (16)
Defining the minimal structural requirements for partial agonism at the type I myo‐inositol 1,4,5‐trisphosphate receptor (1997) (16)
Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transporter inhibitors. (2002) (16)
Synthetic chemistry, neurotransmission and second messengers (1990) (16)
Synthesis of an alleged constituent of New Brunswick cranberry leaves: The so-called cannivonine (1983) (16)
2,3-disubstituted 6-azabicyclo[3.2.1]octanes as novel dopamine transporter inhibitors. (2004) (16)
Simplified analogs of himbacine displaying potent binding affinity for muscarinic receptors (1993) (16)
Borohydride induced cleavage of azo derivatives of β-ketoesters. A useful variant of the Japp-Klingemann reaction for C-nucleoside synthesis. (1978) (16)
Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C. (2001) (16)
IAC Reactions in the Indole Series: Total Synthesis of Clavicipitic Acid (1982) (16)
Block of spatial learning by mG1uR agonist tADA in rats (1995) (16)
The effects of huperzine A and IDRA 21 on visual recognition memory in young macaques (2011) (16)
SYNTHESIS OF THE 6- AND 7-HYDROXYLATED COCAINES AND PSEUDOCOCAINES (1996) (15)
A biomimetic route to the ergot derailment products, the clavicipitic acids - detection of a reactive intermediate by 31p nmr - some chemical underpinnings for a proposed intermediate in ergot alkaloid biosynthesis. (1985) (15)
Mercaptoacetamide: A promising zinc-binding group for the discovery of selective histone deacetylase 6 inhibitors. (2020) (15)
1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties. (1999) (15)
Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. (2017) (15)
Continuous Activity Assay for HDAC11 Enabling Reevaluation of HDAC Inhibitors (2019) (15)
Chemistry, pharmacology, and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile. Part II. (2013) (15)
Meldrum's acid derivative as a useful dienophilic component; Synthesis of δ-damascone (1975) (15)
Use of a thermally stable, optically active nitrile oxide in the synthesis of a lyngbyatoxin A intermediate (1987) (15)
Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors. (2009) (15)
Restoration of TEA-Induced Calcium Responses in Fibroblasts from Alzheimer's Disease Patients by a PKC Activator (1998) (15)
A versatile approach to PI(3,4)P2, PI(4,5)P2, and PI(3,4,5)P3 from L-(-)-Quebrachitol (2000) (15)
Pharmacological studies on novel neurotensin mimetics: discovery of a pharmacologically unique agent exhibiting concentration-dependent dual effects as antagonist and agonist. (1993) (15)
An enantioselective synthesis of 2-alkyl-3-phenyltropanes by an asymmetric 1,3-dipolar cycloaddition reaction (1997) (15)
Total synthesis of the unique indole alkaloid chuangxinmycin. Application of nitro group displacement reactions in organic synthesis [9] (1980) (15)
Tools for Cell Signaling: Synthesis of the 3-Phosphatase-Resistant 1,3,4,5-InsP4 Mimic, 1D-myo-Inositol 1,4,5-Trisphosphate 3-Phosphorothioate (1994) (14)
A [(4 + 2) + (3 + 2)] approach to a forskolin intermediate; a further understanding of π-facial selection in Diels-Alder reactions (1988) (14)
A General Approach to the Pseudopterosins and Their C-11 and C-13 Stereoisomers. Construction of the Tricyclic Skeleton of the Pseudopterosins (1991) (14)
Structure‐Guided Design of a Highly Selective Glycogen Synthase Kinase‐3β Inhibitor: a Superior Neuroprotective Pyrazolone Showing Antimania Effects (2011) (14)
Further structure-activity relationship studies of piperidine-based monoamine transporter inhibitors: effects of piperidine ring stereochemistry on potency. Identification of norepinephrine transporter selective ligands and broad-spectrum transporter inhibitors. (2005) (14)
Probing ergot alkaloid biosynthesis: Identification of advanced intermediates along the biosynthetic pathway (1988) (14)
Synthesis and biological activity of the D-3-deoxy-3-fluoro and D-3-chloro-3-deoxy analogues of phosphatidylinositol (1994) (14)
Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity. (2011) (14)
Efficient Coupling reactions of β-Amino and β-Acetamido Radicals with Electron Deficient Alkenes - Aza-Carbofunctionalization of Olefins - A Promising New Tool for Alkaloid Synthesis. (1983) (14)
The INOC approach to the hydroazulenone ring system - a potential entry tot he guaianolides and pseudoguaianolides. (1983) (14)
The conversion of methyl pseudomonate C to pseudomonic acid A (1981) (14)
An unusually facile thioallylic rearrangement - stereochemical evidence for a free radical chain mechanism (1982) (13)
Oxidation of isoxazolines by peracids - a useful route to β-hydroxy ketones and acylated diols (1988) (13)
An approach to bi-tetrahydrofurans from glucose and a correction of the literature (1987) (13)
1D-myo-inositol 1,4,5-trisphosphate and 1D-myo-inositol 1,3,4,5-tetrakisphosphate analogues modified at C-3; synthesis of 1D-3-C-(trifluoromethyl)-myo-inositol 1,4,5-trisphosphate and 1L-chiro-insitol 1,2,3,5-tetrakisphosphate from L-quebrachitol (1994) (13)
Probing ergot alkaloid biosynthesis : intermediates in the formation of ring C (1993) (13)
SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement. (2002) (13)
Modification of the side chain of micromolide, an anti-tuberculosis natural product. (2008) (13)
Use of molecular modeling, docking, and 3D-QSAR studies for the determination of the binding mode of benzofuran-3-yl-(indol-3-yl)maleimides as GSK-3β inhibitors (2009) (13)
SYNTHESIS OF 2-SUBSTITUTED Δ3-PIPERIDINES: THE NITROGEN ANALOG OF THE FERRIER REARRANGEMENT. AN APPROACH TO STREPTAZOLIN (1984) (13)
An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes. (2000) (12)
Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors. (2002) (12)
The intramolecular nitrile oxide cycloaddition approach to the mitomycins (1988) (12)
Neurobiology of the Nmda Receptor: From Chemistry to the Clinic (1991) (12)
Synthesis, chiral chromatographic separation, and biological activities of the enantiomers of 10,10-dimethylhuperzine A. (2000) (12)
An examination of π-facial selectivity in the diels-alder reaction of a chiral diene - a synthesis of (+)-5,6,10-tri-(EPI)-Actinobolin. (1986) (12)
Mixed Cocaine Agonist/Antagonist Properties of (+)-Methyl 4β-(4-Chlorophenyl)-1-methylpiperidine-3α-carboxylate, a Piperidine-Based Analog of Cocaine (2003) (12)
Deoxygenated inositol 1,4,5-trisphosphate analogues and their interaction with metabolic enzymes. (1R,2R,4R)-cyclohexane-1,2,4-tris(methylenesulfonate): a potent selective 5-phosphatase inhibitor. (1993) (12)
Telescoped continuous flow generation of a library of highly substituted 3-thio-1,2,4-triazoles (2017) (12)
NOC Chemistry for Tuberculosis—Further Investigations on the Structure–Activity Relationships of Antitubercular Isoxazole‐3‐carboxylic Acid Ester Derivatives (2010) (12)
Synthetic studies of the rubradirins. A strategy for the incorporation of the ansa bridge (1987) (12)
Enantioselective deprotonation of the 8-oxabicyclo[3.2.1]octan-3-one: Synthesis of 8-oxa-norcocaines and 8-oxa-pseudonorcocaines (1999) (12)
Design and Synthesis of (2-(5-Chloro-2,2-dimethyl-2,3-dihydrobenzofuran-7-yl)cyclopropyl)methanamine as a Selective Serotonin 2C Agonist. (2015) (12)
The novel Ins(1,4,5)P3 analogue 3-amino-3-deoxy-Ins(1,4,5)P3: a pH-dependent Ins(1,4,5)P3 receptor partial agonist in SH-SY5Y neuroblastoma cells. (1994) (12)
SAR of cocaine: further exploration of structural variations at the C-2 center provides compounds of subnanomolar binding potency (1993) (12)
Exploration of the labeling of [11C]tubastatin A at the hydroxamic acid site with [11C]carbon monoxide. (2016) (12)
Chemistry of the main group metals: A stereoselective synthesis of allyl vinyl thioethers for the thio—claisen reaction (1979) (12)
USE OF THE ANOMERIC ALLYLATION REACTION IN NATURAL PRODUCTS SYNTHESIS ‐ A STEREOCONTROLLED SYNTHESIS OF METHYL DEOXYPSEUDOMONATE B (1984) (11)
Optimization of Drug Candidates That Inhibit the D‐Loop Activity of RAD51 (2019) (11)
The synthesis of 2,3,3a,4,5,7a-hexahydro-1H-inden-1-ols by intramolecular Diels-Alder reactions of 1,3,8-nonatrien-5-ols. Dependence of product stereochemistry on the substitution pattern (1991) (11)
Synthesis of 4-Arylethynyl-2-methyloxazole Derivatives as mGluR5 Antagonists for Use in the Treatment of Drug Abuse (2006) (11)
A PLE-BASED RESOLUTION OF COCAINE, PSEUDOCOCAINE, AND 6- AND 7-METHOXYLATED COCAINE ANALOGUES (1996) (11)
Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles. (2001) (11)
Preparation and reactions of 1-(phenylthio)-2-[(trimethylsilyl)oxy]-1,3-butadienes. A one-pot synthesis of sulfur-substituted 7-hydroxybicyclo[2.2.1]heptanones: Coupling of the Diels-Alder reaction with the aldol process (1982) (11)
The intramolecular nitrile oxide cycloaddition route to spirocyclic alkaloids. A total synthesis of isonitramine and sibirine (1985) (11)
From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design. (2012) (11)
Rational Design and Development of Radiation‐Sensitizing Histone Deacetylase Inhibitors (2005) (11)
Stereochemistry of the alkoxyselenation of substituted 3,4-dihydropyrans: a useful process for the construction of 2-alkoxy-5,6-dihydro-2H-pyrans (1980) (11)
Development of novel amyloid imaging agents based upon thioflavin S. (2005) (11)
Synthesis and biological activity of an optically pure 10-spirocyclopropyl analog of huperzine A (1998) (11)
Functionalization of the alicyclic skeleton of epibatidine: synthesis and nicotinic acetylcholine receptor binding affinities of epibatidine analogues. (2003) (11)
Synthetic Studies on the Stemona Alkaloids; Stereochemical Course of PhSe+ -Induced Seven-Membered Ring Formation (1990) (10)
Synthesis and binding studies of an optically pure hexadeoxy-1,4,5-tris(methylenesulfonic acid) analogue of IP3 (1993) (10)
Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity. (1999) (10)
ORGANIC REACTIONS AT HIGH PRESSURE, CYCLOADDITIONS OF ENAMINES AND DIENAMINES (1974) (10)
Synthesis of 2-alkyl-3-aryl-substituted quinuclidines as novel dopamine transporter inhibitors (2000) (10)
Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors. (2004) (10)
Discrimination of potent inhibitors of Toxoplasma gondii enoyl-acyl carrier protein reductase by a thermal shift assay. (2013) (10)
Preparation of a benzenoid intermediate For use in the synthesis of Maytansine (1977) (10)
Studies directed toward the total synthesis of the rubradirin antibiotics. 2. Synthesis of the unique morpholinonaphthoquinone chromophore: A lesson in Diels-Alder regiocontrol by diene substituent selection [3] (1981) (10)
alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists. (1998) (10)
Clinical and Preclinical Studies with Huperzine (1991) (10)
Synthesis of more potent analogues of the acetylcholinesterase inhibitor, huperzine B. (2002) (10)
Synthesis of methoxy and hydroxy analogues of 1,2,3,4,4a,9a-hexahydro-4a-fluorenamine : rigid phencyclidine analogues as probes of phencyclidine binding site topography (1991) (10)
Synthesis and acetylcholinesterase inhibitory activity of several pyrimidone analogues of huperzine A (1995) (10)
Synthesis and biological activity of 3-hydroxy(phosphono)methyl-bearing phosphatidylinositol ether lipid analogues (2002) (10)
Organometallics in organic synthesis. Applications of a new diorganozinc reaction to the synthesis of C-glycosyl compounds with evidence for an oxonium-ion mechanism. (1987) (10)
Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine. (1999) (10)
Concise Enantioselective Synthesis and Attribution of the Absolute Configuration of Two-Carbon Bridge Methoxylated Cocaines and Pseudococaines (1998) (9)
Probing Ergot Alkaloid Biosynthesis: Intermediates in the Formation of Ring C. (1993) (9)
Advancing the Therapeutic Potential of Indoleamides for Tuberculosis (2019) (9)
Observations regarding eschenmoser sulfide contractions of β-oxygenated thiolactams (1995) (9)
Synthesis and biological evaluation of novel hybrids of highly potent and selective α4β2-Nicotinic acetylcholine receptor (nAChR) partial agonists. (2016) (9)
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands. (2020) (9)
Differential binding and dopamine uptake activity of cocaine analogues modified at nitrogen (1994) (9)
Studies directed toward the total synthesis of the rubradirin antibiotics. 5. A convenient preparation of functionalized isoprene units for the diels-alder reaction (1982) (9)
Natural and Synthetic Huperzine A: Effect on Cholinergic Function in Vitro and in Vivo a (1993) (9)
Design of an irreversible affinity ligand for the phencyclidine recognition site on N-methyl-D-aspartate-type glutamate receptors. (1992) (9)
Synthesis of the First Optically Pure, Fluorinated Inositol 1,4,5‐ Trisphosphate of myo‐Inositol. Stereochemistry and Its Effect on Ca2+ Release in Swiss 3T3 Cells. (1991) (9)
A synthesis of (–)-1L-1-deoxy-1-fluoro-myo-inositol; a compound of potential use in sorting out the phosphatidylinositol response (1988) (9)
Synthesis of Huperzine A (I) and Its Analogues and Their Anticholinesterase Activity. (1991) (9)
A General Route to Homophthalic Acid Derivatives - Valuable Precursors to Isoquinolinones, Dihydronaphthols and Isocoumarins (1978) (9)
Reactivity of 4,6-dioxy-2-pyrones in the Diels-Alder process (1979) (9)
Chemical synthesis and biological evaluation of 1 d-1,2,4,5-InsP 4 and its 3-fluorinated counterpart 1 d-3-F-1,2,4,5-InsP 4 — potent 1 d-1,4,5-InsP 3-like calcium mobilizing analogues (1995) (9)
The synthesis of substituted (4S)-4-(hydroxymethyl)imidazolidin-2-ones as novel protein kinase C modulators (2000) (9)
Synthesis and biological evaluation of two analogues of (S)- α-methyl -3-carboxyphenylalanine (1998) (8)
Synthesis of novel spirocyclic cocaine analogs using the Suzuki coupling (2000) (8)
Synthesis of partial nonpeptidic peptide mimetics as potential neurotensin agonists and antagonists (1995) (8)
Intramolecular azide cycloaddition (IAC) reactions in the indole series - an approach to clavicipitic acid (1982) (8)
Synthesis and metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation. (1998) (8)
Stereoselective HDAC Inhibition from Cysteine‐Derived Zinc‐Binding Groups (2009) (8)
Down regulation of the expression of the p110, p85 and p55 subunits of phosphatidylinositol 3-kinase during colon cancer cell anchorage-independent growth. (1999) (8)
A total synthesis of actinobolin via the intermolecular Diels–Alder reaction of a threonine-derived diene (1986) (8)
Synthesis of 1D-3-Deoxy-, 1D-2,3-Dideoxy-, and 1D-2,3,6-Trideoxy-myo- inositol 1,4,5-Trisphosphate from Quebrachitol, Their Binding Affinities, and Calcium Release Activity. (1993) (8)
[125I]thienylphencyclidine, a novel ligand for the NMDA receptor. (1992) (8)
Acetylenic Pyridines for Use in PET Imaging of Nicotinic Receptors (2007) (8)
Synthesis and Akt inhibitory properties of a 1d-3,4-dideoxyphosphatidylinositol ether lipid (2000) (8)
Synthesis and evaluation of iodine-123 labelled tricyclic tropanes as radioligands for the serotonin transporter. (2003) (8)
N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter. (1999) (8)
USE OF N,N-DIMETHYL(METHYLENE)AMMONIUM CHLORIDE IN THE FUNCTIONALIZATION OF INDOLES (1980) (7)
Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selective α4β2-nAChR Ligands. (2014) (7)
Structural analogs of huperzine A improve survival in guinea pigs exposed to soman. (2013) (7)
Synthesis of the ‘supposed’ cannivonine: a constituent of new brunswick cranberry leaves (1979) (7)
Development of new brain imaging agents based upon nocaine-modafinil hybrid monoamine transporter inhibitors. (2006) (7)
New synthesis of 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I (ABHxD-I), a potent metabotropic receptor agonist (2000) (7)
Radical cyclization strategies for the formation of ring constrained tricyclic tropane analogues (2000) (7)
Synthesis and 2D NMR analysis of a cyclopropane containing analogue of huperzine A (1992) (7)
Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors. (2003) (7)
Synthesis of N1-substituted analogues of (2R,4R)-4-amino-pyrrolidine-2,4-dicarboxylic acid as agonists, partial agonists, and antagonists of group II metabotropic glutamate receptors (2001) (7)
Structural determinants of affinity for the phencyclidine binding site of the N-methyl-D-aspartate receptor complex: discovery of a rigid phencyclidine analogue of high binding affinity. (1990) (7)
An approach to the construction of the aromatic portions of naphthomycin and the rubradirins - nucleophilic additions to unsymmetrically substituted naphthoquinones (1980) (7)
Synthesis of 1D-3-deoxy- and -2,3-dideoxyphosphatidylinositol (1997) (7)
Neurochemistry of aging. 2. Design, synthesis, and biological evaluation of halomethyl analogues of choline with high affinity choline transport inhibitory activity. (1991) (7)
Synthesis of 7-methoxybenzolactam-V8 using a diastereoselective Strecker synthesis (2001) (7)
Synthesis of D-3-deoxy-3-phosphonomethyl-myo-inositol and its dimethyl ester - compounds of use in studying the ptdins-3′-kinase signalling pathway (1993) (7)
Synthesis and Behavioral Studies of Chiral Cyclopropanes as Selective α4β2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile. Part III. (2016) (7)
2,3-Disubstituted quinuclidines as a novel class of dopamine transporter inhibitors. (2003) (7)
Expedient synthetic routes to [3H]-D-3-azido-3-deoxy-myo-inositol and D-3-azido-3-deoxy-myo-inositol 2,4,5-trisphosphate (1992) (7)
OXAZOLES IN ORGANIC CHEMISTRY. SYNTHESIS OF THE ANTITUMOR AGENT ELLIPTICINE (1977) (7)
Synergistic Interactions of Indole-2-Carboxamides and β-Lactam Antibiotics against Mycobacterium abscessus (2020) (6)
Studies directed toward the total synthesis of the rubradirin antibiotics. 4. A new Diels-Alder—Claisen effective diene (1981) (6)
Synthesis and modeling study of (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy- 8-(1-decynyl)-benzolactam-V8 as protein kinase C modulators. (2002) (6)
Metalation of 2,2-dimethyl-5-methylene-1,3-dioxane---a functionalized allyloxy carbanion. (1979) (6)
Synthesis of novel metabolically stable analogues of D-myo-inositol 1,4,5-trisphosphate (1996) (6)
PREPARATION AND REACTIONS OF 1-(PHENYLTHIO)-2-(TRIMETHYLSILYLOXY)-1,3-BUTADIENES. A ONE-POT SYNTHESIS OF SULFUR-SUBSTITUTED 7-HYDROXYBICYCLO(2.2.1)HEPTANONES - COUPLING OF THE DIELS-ALDER REACTION WITH THE ALDOL PROCESS (1982) (6)
SYNTHESIS OF CYCLIC SPHINGOSINE 1,3-PHOSPHATE (CSPP) THROUGH A PHOTOLYTIC REACTION (1998) (6)
Variation of CS salience reveals group II mGluR-dependent and -independent forms of conditioning in the rat (2002) (6)
A derivative of a rigid glutamate analog protects the retina from excitotoxicity. (1994) (6)
Structural Remodeling of Cocaine: Design and Synthesis of Trisubstituted Cyclopropanes as Selective Serotonin Reuptake Inhibitors (2006) (6)
Neuroprotective and Cognitive Enhancing Effects of Novel Small Peptides (1999) (6)
Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine. (2000) (6)
A convenient procedure for the synthesis of nonsymmetrical bivalent selective serotonin reuptake inhibitors using polymer-supported reagents. (2000) (5)
Synthesis of (2-Arylindol-3-yl)acetamides as Probes of Mitochondrial Steroidogenesis—A New Mechanism for GABAA Receptor Modulation† (1992) (5)
Probing the D-1,4,5-IP3/D-1,3,4,5-IP4 functional interface. Synthesis and pharmacology of novel D-3-modified myo-inositol trisphosphate analogues (1994) (5)
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model. (2021) (5)
Use in the Synthesis of Non-heterocycles (1984) (5)
A palladium catalyzed route to a benzofuran analogue of idolactam V (ILV): Effects on PKC isotype selectivity (1994) (5)
Synthesis and Protein Kinase C Binding Activity of Benzolactam‐V7. (1999) (5)
Synthesis of the 2β,3β-, 2α,3β-, 2β,3α- and 2α,3α- isomers of 6β-hydroxy-3-(p-tolyl)tropane-2-carboxylic acid methyl ester (1999) (5)
Stereochemistry at the forefront in the design and discovery of novel anti-tuberculosis agents. (2011) (5)
Synthesis and biological activity of new 6- and 7-substituted 2β- butyl-3-phenyltropanes as ligands for the dopamine transporter (1998) (5)
Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors. (2000) (5)
Erratum: Dopaminergic agents for the treatment of cocaine abuse (Drug Discovery Today (1999) issue 7, (322-332)) (1999) (5)
THE INOC ROUTE TO CARBOCYCLICS: A FORMAL TOTAL SYNTHESIS OF (.+-.)-SARKOMYCIN (1982) (5)
Synthesis and biological activity of 8a-phenyldecahydroquinolines as probes of PCP's binding conformation. A new PCP-like compound with increased in vivo potency. (1992) (5)
TOTAL SYNTHESIS OF THE UNIQUE INDOLE ALKALOID CHUANGXINMYCIN. APPLICATION OF NITRO GROUP DISPLACEMENT REACTIONS IN ORGANIC SYNTHESIS (1980) (5)
Conjugative additions of allyl ylids to dienoic esters: A new synthesis of bicyclo[4.1.0]heptenes. (1973) (5)
A New Indole Synthesis Promoted by Metal Triflates (1986) (5)
THE ((4 + 2) + (3 + 2)) ROUTE TO MULTIPLY FUSED RING SYSTEMS: A NEW NOTION IN POLYCYCLE CONSTRUCTION (1984) (5)
Synthesis and Biology of the Rigidified Glutamate Analogue, trans-2- Carboxyazetidine-3-acetic Acid (t-CAA). (2010) (4)
A versatile approach to PI(3,4)P2, PI(4,5)P2, and PI(3,4,5)P3 from L-(-)-quebrachitol. (2000) (4)
Chemical Modification of Ring C of Himbacine: Discovery of a Pharmacophoric Element for M2-Selectivity. (1995) (4)
Radiolabeling and biodistribution of methyl 2-(methoxycarbonyl)-2-(methylamino) bicyclo[2.1.1] -hexane -5-carboxylate, a potential neuroprotective drug. (2003) (4)
A Practical Synthesis of the Chinese “Nootropic” Agent Huperzine A: A Possible Lead in the Treatment of Alzheimer′s Disease. (1989) (4)
Studies directed toward the total synthesis of the rubradirin antibiotics. 3. Diels-alder reactions of unsymmetrically substituted quinones-a confirmation of structure. (1980) (4)
SYNTHESIS OF 4-SUBSTITUTED INDOLES AND THEIR ELABORATION TO THE ERGOT ALKALOIDS (1981) (4)
Cellular pharmacology ofd-3-azido-3-deoxy-myo-inositol, an inhibitor of phosphatidylinositol signaling having antiproliferative activity (2004) (4)
Therapeutic Potential Of Selective Inhibition Of Histone Deacetylase 6 (hdac6) In Different Forms Of Cmt2 (2015) (4)
2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics. (2018) (4)
Synthesis of Novel Four‐Membered Ring Amino Acids as Modulators of the N‐Methyl‐D‐aspartate (NMDA) Receptor Complex. (1992) (4)
Synthesis of partially non-peptidic neurotensin mimetics (1994) (4)
An unusual fragmentation process discovered during the course of cleavage of a camphanic acid amide (1990) (4)
Design, Synthesis, and SAR Studies of Mefloquine‐Based Ligands as Potential Antituberculosis Agents (2006) (4)
Abstract 2699: Targeting GSK-3: a novel approach to enhance glioblastoma chemosensitivity (2015) (3)
Topography of the huperzine A binding site in AChE: Ab initio docking of reversible inhibitors of AChE into the dynamic enzyme (1993) (3)
The potent and selective α4β2*/α6*-nicotinic acetylcholine receptor partial agonist 2-[5-[5-((S)Azetidin-2-ylmethoxy)-3-pyridinyl]-3-isoxazolyl]ethanol demonstrates antidepressive-like behavior in animal models and a favorable ADME-tox profile (2014) (3)
Synthesis and Evaluation of a Photolyzable Derivative of Sphingosine 1-Phosphate—Caged SPP. (1998) (3)
Synthesis and Pharmacological Evaluation of (Z)‐9‐(Heteroarylmethylene)‐7‐azatricyclo[4.3.1.03,7]decanes: Thiophene Analogues as Potent Norepinephrine Transporter Inhibitors. (2004) (3)
Rational design of novel neurotensin mimetics: Discovery of a pharmacologically unprecedented agent exhibiting concentration-dependent dual effects as antagonist and full agonist (1994) (3)
Novel monoamine transporter ligands reduce cocaine-induced enhancement of brain stimulation reward (2001) (3)
Novel Glycogen Synthase Kinase 3beta Inhibitors Induce Apoptosis in Ovarian Cancer. (2010) (3)
Synthesis of 7‐Substituted Benzolactam‐V8s and Their Selectivity for Protein Kinase C Isozymes. (2002) (3)
The preclinical candidate indole-2-carboxamide improves immune responses to Mycobacterium tuberculosis infection in healthy subjects and individuals with type 2 diabetes (2020) (3)
Synthesis of N-[1-(2-Thienyl)cyclohexyl]piperidine (TCP) Based Irreversible Alkylators of the Phenylcyclidine (PCP) Recognition Site (1991) (3)
Neuroprotective effects of the agonist of metabotropic glutamate receptors ABHxD-I in two animal models of cerebral ischaemia. (2006) (3)
Methods for Synthesizing the Cocoa‐Derived Oligomeric Epi‐Catechins – Observations on the Anticancer Activity of the Cocoa Polyphenols (2009) (3)
Chemical medicine: novel 10-substituted cytisine derivatives with increased selectivity for alpha4beta2 nicotinic acetylcholine receptors. (2007) (3)
ATPS-91GSK-3 INHIBITOR 9-ING-41 ENHANCES GENOTOXIC THERAPY OF GBM LEADING TO CURE FROM INTRACRANIAL BRAIN TUMOR. (2015) (2)
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT2C) receptor agonist without 5-HT2B agonism. (2019) (2)
A General Approach to the Pseudopterosins and Their C-11 and C-13 Stereoisomers. Construction of the Tricyclic Skeleton of the Pseudopterosins. (1992) (2)
1,3-DIETHOXYCARBONYLALLENE- AN ACTIVE DIENOPHILE AND ETHOXYCARBONYLKETENE EQUIVALENT IN THE SYNTHESIS OF ANTIBIOTIC C-NUCLEOSIDES (1978) (2)
Synthesis and Chemical Resolution of a Novel Class of Rigid 1-(1-Phenylcyclohexyl)-iperidine(PCP) Analogues (1990) (2)
Pharmacokinetics and brain penetration of LF-3-88, (2-[5-[5-(2(S)-azetidinylmethoxyl)-3-pyridyl]-3-isoxazolyl]ethanol), a selective α4β2-nAChR partial agonist and promising antidepressant. (2013) (2)
The Discovery of New Chemical Modulators of the N‐Methyl‐D‐Aspartate Receptor (1989) (2)
Synthesis, biodistribution, and experimental prostate tumor imaging of p-[125I]iodobenzoyl-lys-NH(CO)NH-glu (2007) (2)
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants. (2005) (2)
Synthesis of the Indole Alkaloid α-Cyclopiazonic Acid (αCA) by Two Sulfur-Mediated Reactions: Discovery of a Useful Diorganozinc Reaction (1989) (2)
Synthesis and evaluation of 99mTc/Re labeled PSMA inhibitors (2007) (2)
Small Cell Lung Cancer Cells − LKB 1-Mutant Non Dependent Death in − AMP-Activated Protein Kinase Phosphatidylinositol Ether Lipid Analogues Induce (2008) (2)
Synthesis of 4-Arylethynyl-2-methyloxazole Derivatives as mGluR5 Antagonists for Use in the Treatment of Drug Abuse. (2006) (2)
Effect of alteration of the heterocyclic nucleus of ILV on its isoform selectivity for PKC. Palladium catalyzed route to benzofuran analogues of ILV. (1995) (2)
A Simplified Route to a Key Intermediate in the Synthesis of the Chinese Nootropic Agent Huperzine A. (1990) (2)
Synthesis of a biotin conjugate of the PCP analogue “metaphit” for potential use in NMDA/PCP receptor isolation (1989) (2)
Erratum: Peroxisome proliferator-activated receptor δ and γ agonists differentially alter tumor differentiation and progression during mammary carcinogenesis (Cancer Research (May 1, 2005) 65 (3950-3957)) (2005) (2)
Synthesis and biological evaluation of two analogues of (S)-alpha-methyl-3-carboxyphenylalanine. (1998) (2)
Glycogen Synthase Kinase-3 Inhibition Sensitizes Pancreatic Cancer Cells to Chemotherapy by Abrogating the TopBP 1 / ATR-Mediated DNA Damage Response (2019) (2)
Effective Collaborations: How to Protect Yourself, Your Collaborators, and Your Data (2011) (2)
Synthesis of the benzofuran analogue of ILV, a new protein kinase C(PKC) activator (1994) (2)
Abstract LB-295: A novel regulatory role of HDAC6 in the functional inflammatory phenotype of glia cells (2017) (1)
NOC APPROACH TO SPIROKETALS. A TOTAL SYNTHESIS OF (.+-.)-TALAROMYCIN B (1984) (1)
The Synthesis of Tricyclic Cocaine Analogues via the 1,3-Dipolar Cycloaddition of Oxidopyridinium Betaines. (1998) (1)
Synthesis and Biological Activity of the D-3-Deoxy-3-fluoro and D-3- Chloro-3-deoxy Analogues of Phosphatidylinositol. (1994) (1)
An Improved Synthetic Route to Huperzine A. New Analogues and Their Inhibition of Acetylcholinesterase. (1993) (1)
Inhibition of Histone Deacetylase 6 (HDAC6) Disrupts the Tolerogenic STAT3 Signaling Pathway and Augments Antitumor Immune Responses in Mantle Cell Lymphoma (MCL) (2012) (1)
Ether Lipid Analogues Cancer Cells by Rationally Designed Phosphatidylinositol Preferential Inhibition of Akt and Killing of Akt-Dependent (2004) (1)
Radical Cyclization Strategies for the Formation of Ring Constrained Tricyclic Tropane Analogues. (2000) (1)
OXAZOLES IN ORGANIC SYNTHESIS- SOME OBSERVATIONS ON THE USE OF 5-ALKOXYOXAZOLES IN THE DIELS-ALDER PROCESS (1978) (1)
AN EXAMINATION OF THE EXTENT OF DIASTEREOFACIAL SELECTION IN THE REACTIONS OF A CHIRAL NITRILE OXIDE WITH ACHIRAL ALKENES: A ROUTE TO β-HYDROXY CARBOXYLIC ACIDS (1984) (1)
Synthesis and Biological Activity of Cyclic Analogues of MPPG and MCPG as Metabotropic Glutamate Receptor Antagonists. (1997) (1)
On the path from chemistry to neuroscience: early explorations in chemical medicine under the mentorship of Dr. Erminio Costa, a neuroscientist with a big brain and a bigger heart. (2011) (1)
Positron-emitting PSMA inhibitors for molecular imaging of prostate cancer (2008) (1)
Chemistry and biology of the 2 beta-alkyl-3 beta-phenyl analogues of cocaine: subnanomolar affinity ligands that suggest a new pharmacophore model at the C-2 position. (1995) (1)
Synthesis of (2‐Arylindol‐3‐yl)acetamides as Probes of Mitochondrial Steroidogenesis. A New Mechanism for GABAA Receptor Modulation. (1992) (1)
Filling the pipeline for neglected diseases: creation of a medicinal chemistry-centric international drug discovery institute [iDDi]. (2008) (1)
Synthesis and Acetylcholinesterase Inhibitory Activity of Several Pyrimidone Analogues of Huperzine A. (1995) (1)
General and Stereospecific Route to 9-Substituted, 8,9-Disubstituted, and 9,10-Disubstituted Analogues of Benzolactam-V8. (2000) (1)
Abstract 48: Targeting HDAC6 to reduce the aggressiveness of metastatic breast cancer in immunotherapy (2018) (1)
SAR Studies of Piperidine-Based Analogues of Cocaine. Part 3. Oxadiazoles. (2001) (1)
Targeting the Number Two Infectious Disease Killer--Tuberculosis (2015) (1)
Inhibition of cholinesterases by stereoisomers of Huperzine-A (1993) (1)
Oxidation of Isoxazolines by Peracids. A Useful Route to β-Hydroxy Ketones and Acylated Diols. (1989) (1)
Recent Developments In Novel Antidepressants Targeting Ã”Â±4Ã”Â22-Nicotinic Acetylcholine Receptors (2021) (1)
Abstract 4854: Evaluating HDAC6 as a causal factor in metastatic breast cancer to develop immunotherapy (2017) (1)
Book Review: Carbohydrates—Synthetic Methods and Applications in Medicinal Chemistry. Edited by H. Ogura, A. Hasegawa and T. Suami (1994) (1)
Structure-Based Design of a New Class of Protein Kinase C Modulators. (1998) (1)
Selectivity of Hydroxamate- and Difluoromethyloxadiazole-Based Inhibitors of Histone Deacetylase 6 In Vitro and in Cells (2023) (1)
Mixed cocaine agonist/antagonist properties of (+)-methyl 4beta-(4-chlorophenyl)-1-methylpiperidine-3alpha-carboxylate, a piperidine-based analog of cocaine. (2003) (1)
α‐Substituted Quisqualic Acid Analogues: New Metabotropic Glutamate Receptor Group II Selective Antagonists. (1998) (1)
Physical Interaction of Histone Deacetylase 6 (HDAC6) with STAT3 Regulates IL-10 Gene Expression and Immune Tolerance Mediated by Antigen-Presenting Cells (APCs) (2012) (1)
Applications of Organosulfur Chemistry to Organic Synthesis: Total Synthesis of (+)-Himbeline and (+)-Himbacine. (1997) (1)
Histone deacetylase 6 inhibition improves memory and reduces total tau levels in a mouse model of tau deposition (2014) (1)
THE NITRILE OXIDE CYCLOADDITION (NOC) ROUTE TO A MULTIPURPOSE C-NUCLEOSIDE INTERMEDIATE. A NEW CLASS OF C-NUCLEOSIDES (1983) (1)
Histone/protein deacetylase 11 targeting promotes Foxp3+ Treg function (2017) (1)
STUDIES DIRECTED TOWARD THE TOTAL SYNTHESIS OF THE RUBRADIRIN ANTIBIOTICS. 2. YNTHESIS OF THE UNIQUE MORPHOLINONAPHTHOQUINONE CHROMOPHORE: A LESSON N DIELS-ALDER REGIOCONTROL BY DIENE SUBSTITUENT SELECTION (1981) (0)
Synthesis and Akt Inhibitory Properties of a 1D‐3,4‐Dideoxyphosphatidylinositol Ether Lipid. (2000) (0)
Method for the inhibition of heregulin and its receptor as well as use in inhibiting cancer cells (1997) (0)
Total Synthesis of Chanoclavine I (1981) (0)
EFFICIENT COUPLING REACTIONS OF β-AMINO AND β-ACETAMIDO RADICALS WITH ELECTRON DEFICIENT ALKENES. AZA-CARBOFUNCTIONALIZATION OF OLEFINS. A PROMISING NEW TOOL FOR ALKALOID SYNTHESIS (1983) (0)
The Isoxazoline Route to the Hypocholesterolemic Agent Compactin (I): Use of the Isoxazoline as a 1,3-Diene Equivalent. (1988) (0)
Inhibiteurs du cycle phosphatidyl myo-inositol (1999) (0)
INTRAMOLECULAR AZIDE CYCLOADDITION (IAC) REACTIONS IN THE INDOLE SERIES. AN APPROACH TO CLAVICIPITIC ACID (1982) (0)
Palladium-Catalyzed Synthesis of Anellated Indoles. (1992) (0)
Abstract 2331: HDAC6, new role as master regulator of PD-L1 and immune-related pathways (2016) (0)
An Approach to Bi-tetrahydrofurans from Glucose and a Correction of the Literature. (1987) (0)
CCDC 151517: Experimental Crystal Structure Determination (2001) (0)
Chemistry of Baker′s Yeast Reduction Products: Use of Optically Active (S)-(+)-1-(p-Toluenesulfonyl)propan-2-ol and (S)-(+)-1-(Phenylsulfonyl)propan-2-ol in Synthesis. (1987) (0)
The nAChR agonist AMOP-H-OH (‘sazetidine-A’) exhibits reinforcing, but not withdrawal-alleviating, properties in rats (2009) (0)
A new approach to the modulation of GABA(A) receptors (1993) (0)
Correction: Glycogen Synthase Kinase-3 Inhibition Sensitizes Pancreatic Cancer Cells to Chemotherapy by Abrogating the TopBP1/ATR–mediated DNA Damage Response (2021) (0)
Differential Binding and Dopamine Uptake Activity of Cocaine Analogues Modified at Nitrogen. (1994) (0)
Copper(I) promoted acylation reactions. A transition metal mediated version of the Friedel-Crafts reaction (1980) (0)
Synthesis and Biological Activity of D‐3‐Deoxy‐3‐ fluorophosphatidylinositol ‐ A New Direction in the Design of Non‐DNA Targeted Anticancer Agents. (1993) (0)
Authors Profile (2010) (0)
DIMETHYLALUMINUM METHYLSELENOLATE- A REMARKABLE REAGENT FOR THE PREPARATION OF ACTIVE ACYL-TRANSFER AGENTS (1978) (0)
1-Amino-APDC, a Partial Agonist of Group II Metabotropic Glutamate Receptors with Neuroprotective Properties (1999) (0)
A NOVEL HISTONE DEACETYLASE 6 (HDAC6) INHIBITOR TO MITIGATE TAU PATHOLOGY IN ALZHEIMER’S DISEASE (2019) (0)
A Useful Method for Converting Secondary Alcohols to Their Chlorides with Retention of Configuration. (1988) (0)
Observations Regarding Eschenmoser Sulfide Contractions of β‐ Oxygenated Thiolactams. (2010) (0)
Synthesis of the 2β,3β-, 2α,3β-, 2β,3α-, and 2α,3α-Isomers of 6β-Hydroxy-3-(p-tolyl)tropane-2-carboxylic Acid Methyl Ester. (1999) (0)
Abstract 3555: Histone deacetylase 6 as a novel regulator of the immunogenicity and aggressiveness of melanoma (2012) (0)
Tubastatin A, a Selective HDAC6 Inhibitor, Enhances Antigen-Presenting Cell (APC) Function and Restores the Responsiveness of Anergic CD4+ T Cells (2011) (0)
The Synthesis of 2,3,3a,4,5,7a-Hexahydro-1H-inden-1-ols by Intramolecular Diels-Alder Reactions of 1,3,8-Nonatrien-5-ols. Dependence of Product Stereochemistry on the Substitution Pattern. (1991) (0)
A Palladium‐Catalyzed Route to Huperzine A and Its Analogues and Their Anticholinesterase Activity. (2010) (0)
Synthesis and Pharmacological Evaluation of 8- and 9-Substituted Benzolactam-V8 Derivatives as Potent Ligands for Protein Kinase C, a Therapeutic Target for Alzheimer′s Disease. (2006) (0)
Probing the Topography of Kainate Recognition Sites: Synthesis of a Novel Oxetane‐Containing Kainic Acid Analogue. (1991) (0)
Dipolar Cycloaddition Route to Diverse Analogues of Cocaine: The 6‐ and 7‐Substituted 3‐Phenyltropanes. (1997) (0)
Abstract 2019: Enhancing the effect of immunotherapy by inhibiting tumor promoting effect of HDAC6 (2019) (0)
CONJUGATIVE ADDITIONS OF ALLYL YLIDS TO DIENOIC ESTERS, A NEW SYNTHESIS OF BICYCLO(4,1,0)HEPTENES (1973) (0)
Erratum: Diastereofacial selection in nitrile oxide cycloaddition reactions. The anti-directing effect of an allylic oxygen and some new results on the ring metalation of isoxazolines. A synthesis of (±)-blastmycinone (Journal of Organic Chemistry (1984) 49, 25, (2771)) (1984) (0)
STUDIES DIRECTED TOWARD THE TOTAL SYNTHESIS OF THE RUBRADIRIN ANTIBIOTICS. 4. NEW DIELS-ALDER-CLAISEN EFFECTIVE DIENE (1982) (0)
Synthesis of Fluorine‐Containing Isosters of Sphingosine as Inactivators of Protein Kinase C. (1991) (0)
STUDIES DIRECTED TOWARD THE TOTAL SYNTHESIS OF THE RUBRADIRIN ANTIBIOTICS. 5. CONVENIENT PREPARATION OF FUNCTIONALIZED ISOPRENE UNITS FOR THE DIELS-ALDER DER REACTION (1982) (0)
A Novel Role for Histone Deacetylase 6 (HDAC6) in the Regulation of IL-10 and Immune Tolerance Mediated by Antigen-Presenting Cells (APCs). (2009) (0)
Characterization of C-10 Substituted Analogues of Huperzine A as Inhibitors of Cholinesterases (1998) (0)
Conversion of Alcohols to Protected Guanidines Using the Mitsunobu Protocol. (1994) (0)
Synthesis of the Benzenoid Analogue of the Chinese Nootropic Agent Huperzine A. (1990) (0)
Synthesis and Biological Studies of Simplified Analogues of Lyngbyatoxin A: Use of an Isoxazoline-Based Indole Synthesis. Quest for Protein Kinase C Modulators. (1989) (0)
MELDRUM′S ACID DERIVATIVE AS A USEFUL DIENOPHILIC COMPONENT, SYNTHESIS OF DELTA‐DAMASCONE (1975) (0)
Synthesis and Chemical Resolution of a Novel Class of Rigid 1-(1-Phenylcyclohexyl)piperidine (PCP) Analogues. (1990) (0)
Synthesis of 2‐Alkyl‐3‐aryl‐substituted Quinuclidines as Novel Dopamine Transporter Inhibitors. (2001) (0)
STUDIES DIRECTED TOWARD THE TOTAL SYNTHESIS OF THE RUBRADIRIN ANTIBIOTICS. 3. IELS-ALDER REACTIONS OF UNSYMMETRICALLY SUBSTITUTED QUINONES. A CONFIRMATION OF STRUCTURE (1981) (0)
Synthesis of (.+-.)-10,10-Dimethylhuperzine A - A Huperzine Analogue Possessing a Slower Enzyme Off-Rate. (1996) (0)
Synthese de procyanidines derivees d'epicatechine et de catechine oligomeres (2003) (0)
Abstract LB-074: Priming the tumor microenvironment with epigenetic modifiers to overcome resistance to immune checkpoint inhibitors (2019) (0)
The Intramolecular Nitrile Oxide Cycloaddition Approach to the Mitomycins. (1988) (0)
CHEMISTRY OF THE MAIN GROUP METALS: A STEREOSELECTIVE SYNTHESIS OF ALLYL VINYL THIOETHERS FOR THE THIO-CLAISEN REACTION (1979) (0)
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects in Open Field, Prepulse Inhibition, and Cognition Models (2021) (0)
An Enantioselective Synthesis of 2‐Alkyl‐3‐phenyltropanes by an Asymmetric 1,3‐Dipolar Cycloaddition Reaction. (1998) (0)
Chemistry and Biology of the 2β-Alkyl-3β-phenyl Analogues of Cocaine: Subnanomolar Affinity Ligands that Suggest a New Pharmacophore Model at the C-2 Position. (2010) (0)
Synthetic Studies of the Rubradirins: A Strategy for the Incorporation of the Ansa Bridge. (1987) (0)
Monoclonal antibodies against a phencyclidine derivative are used to investigate protein-ligand interactions. (1993) (0)
Synthesis and Biological Evaluation of (.+‐.)‐Z‐Huperzine A (I). (1991) (0)
Synthesis of a Hybrid Analogue (I) of the Acetylcholinesterase Inhibitors Huperzine A and Huperzine B. (2001) (0)
A FACILE SYNTHESIS OF SUBSTITUTED CONJUGATED CYCLOHEXADIENES (1974) (0)
Synthesis and Biological Activity of an Optically Pure 10‐Spirocyclopropyl Analogue of Huperzine A. (1998) (0)
Use of a Thermally Stable, Optically Active Nitrile Oxide (I) in the Synthesis of a Lyngbyatoxin A Intermediate (II). (1987) (0)
Total Synthesis of Streptazolin: Application of the Aza Analogue of the Ferrier Rearrangement. (1985) (0)
Structure of human PDK1 kinase domain in complex with LY333531 (2004) (0)
METHODS FOR THE STEREOSELECTIVE CIS-CYANOHYDROXYLATION AND -CARBOXYHYDROXYLATION OF OLEFINS (1983) (0)
Abstract 1941: GSK3 signaling is critical to glioma stem cell growth and survival (2014) (0)
METALATION OF 2,2‐DIMETHYL‐5‐METHYLENE‐1,3‐DIOXANE. A FUNCTIONALIZED ALLYLOXY CARBANION (1979) (0)
New Synthesis of 2-Aminobicyclo[2.1.1]hexane-2,5-dicarboxylic Acid-I (ABHxD-I), a Potent Metabotropic Receptor Agonist. (2000) (0)
SYNTHESE DE 4α-ARYLEPICATECHINES (2001) (0)
Development of Small Molecules that Specifically Inhibit the D-loop Activity of RAD51 (2016) (0)
Pharmacophore‐Based Discovery, Synthesis, and Biological Evaluation of 4‐Phenyl‐1‐arylalkyl Piperidines as Dopamine Transporter Inhibitors. (2001) (0)
Synthesis of D‐3‐Deoxy‐myo‐inositol 1,4,5‐Triphosphate and Its Effect of Ca2+ Release in NIH 3T3 Cells. (1991) (0)
Design, synthesis, and pharmacology of novel mGluR ligands . (1999) (0)
Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]Octanes As Selective Ã”Â±4Ã”Â22-Nachr Ligands (2021) (0)
Abstract 960: Ceramide-dependent release of nanovesicles is a class effect oflipid-based Akt inhibitors (2011) (0)
Novel TRH analog improves motor and cognitive recovery after traumatic brain injury in rodents. (1999) (0)
Organometallics in Organic Synthesis: A New Diorganozinc Reaction (1990) (0)
Synthesis of N1-Substituted Analogues of (2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic Acid as Agonists, Partial Agonists, and Antagonists of Group II Metabotropic Glutamate Receptors. (2001) (0)
CCDC 151516: Experimental Crystal Structure Determination (2001) (0)
Composes inhibitant selectivement les lymphocytes t gamma 9 delta 2 (2000) (0)
CCDC 151513: Experimental Crystal Structure Determination (2002) (0)
Modulateurs de pkc a base de pyrrolidone rigide (2001) (0)
Synthesis and Pharmacological Characterization of Bivalent Ligands of Epibatidine at Neuronal Nicotinic Acetylcholine Receptors (2004) (0)
Production method of Huperzine A and its analogues and compounds useful to (1990) (0)
A New Indole Synthesis Promoted by Metal Triflates. (1987) (0)
π-Facial Selection in Intermolecular Diels-Alder Reactions: Total Syntheses of (+)-Actinobolin and (+)-5,6,10-triepi-Actinobolin. (1987) (0)
Probing the functions of NAAG via NAAG peptidases and MGLUR3 (2008) (0)
Specific ligands of the peripheral benzodiazepine receptor decrease proliferation of colorectal cancer cells by induction of apoptosis and cell cycle arrest (2001) (0)
Probing Ergot Alkaloid Biosynthesis: Synthesis and Feeding of a Proposed Intermediate Along the Biosynthetic Pathway. A New Amidomalonate for Tryptophan Elaboration. (1988) (0)
BIS-(DIMETHYLALUMINUM)1,3-PROPANEDITHIOLATE - A USEFUL REAGENT IN THE CONVERSION OF ESTERS TO UNSATURATED ALDEHYDES AND KETONES (1975) (0)
Phosphoniosilylation: An Efficient and Practical Method for the β-Functionalization of Enones. (1987) (0)
A Simplified Route to the Phosphatidylinositol Cascade Inhibitor. L-(-)-1-Deoxy-1-fluoro-myo-inositol. (1990) (0)
Neurochemistry of Aging. Part 2. Design, Synthesis, and Biological Evaluation of Halomethyl Analogues of Choline with High Affinity Choline Transport Inhibitory Activity. (1991) (0)
A Synthesis of (-)-1L-1-Deoxy-1-fluoro-myo-inositol (I). A Compound of Potential Use in Sorting out the Phosphatidylinositol Response. (1989) (0)
Cellular Sensitization to m-Diamminedichloroplatinum(II) by Novel Analogues of the Protein Kinase C Activator Lyngbyatoxin A1 (2006) (0)
ORGANOMETALLIC COMPOUNDS IN ORGANIC SYNTHESIS: NUCLEOPHILIC SUBSTITUTION REACTIONS OF N‐METHYLINDOLETRICARBONYLCHROMIUM(0) (1979) (0)
Construction of Optically Pure Tryptophans from Serine-Derived Aziridine-2-carboxylates. (1990) (0)
Abstract B068: Inhibition of GSK-3: A novel therapeutic approach for breast cancer treatment (2013) (0)
Design, synthesis, and biological evaluation of novel constrained tropane analogs (2000) (0)
Intramolecular [3 + 2] cycloaddition reactions in the indole series "The nitrile oxide route to the ergot alkaloids". 1. Chanoclavine I (1980) (0)
A Model Study for the Synthesis of the Tumor Promoting Agents Lyngbyatoxin A and Teleocidin B. (1986) (0)
Dimethylaluminum Methaneselenolate: A Useful Reagent for the Preparation of Selenoesters. (1986) (0)
DM50, A NOVEL SYNTHETIC PROTEIN KINASE C MODULATOR, INHIBITS LYMPHOCYTE PROLIFERATION AND PROLONGS MURINE CARDIAC ALLOGRAFT SURVIVAL. (1999) (0)
Enantioselective Deprotonation of the 8-Oxabicyclo[3.2.1]octan-3-one: Synthesis of 8-Oxa-norcocaines and 8-Oxa-pseudonorcocaines. (1999) (0)
A Tandem Michael Addition Ring-Closure Route to the Metabotropic Receptor Ligand α-(Hydroxymethyl)glutamic Acid (IV) and Its γ-Alkylated Derivatives. (2002) (0)
Abstract PR02: Small molecules that specifically inhibit the D-loop activity of RAD51 (2017) (0)
SYNTHESIS OF THE 2BETA , -3BETA -, 2ALPHA , 3BETA -, 2BETA , 3ALPHA - AND 2ALPHA , 3ALPHA - ISOMERS OF 6BETA -HYDROXY-3-(P-TOLYL)TROPANE-2-CARBOXYLIC ACID METHYL ESTER (1999) (0)
Synthesis and Biological Evaluation of Two Analogues of (S)‐α‐Methyl‐3‐carboxyphenylalanine. (1999) (0)
Synthesis of 7-Methoxybenzolactam-V8 Using a Diastereoselective Strecker Synthesis. (2001) (0)
TOTAL SYNTHESIS OF THE UNIQUE MYCOTOXIN α-CYCLOPIAZONIC ACID (αCA): AN UNUSUAL DIMETHYLZINC MEDIATED REPLACEMENT OF A PHENYLTHIO SUBSTITUENT BY METHYL GROUP AND A CONTRATHERMODYNAMIC RANEY NICKEL DESULFURIZATION REACTION (1985) (0)
Analogues d'huperzine a (1992) (0)
An Efficacious Synthesis of Aryl and Heteroaryl C-Glycosides. (1987) (0)
Synthesis of Cyclic Sphingosine 1,3-Phosphate (cSPP) Through a Photolytic Reaction. (1999) (0)
The Synthesis of Substituted (4S)-4-(Hydroxymethyl)imidazolidin-2-ones as Novel Protein Kinase C Modulators. (2001) (0)
AN APPROACH TO THE CONSTRUCTION OF THE AROMATIC PORTIONS OF NAPHTHOMYCIN AND THE RUBRADIRINS. NUCLEOPHILIC ADDITIONS TO UNSYMMETRICALLY SUBSTITUTED NAPHTHOQUINONES (1980) (0)
Synthesis of 1D-3-Deoxy- and -2,3-Dideoxyphosphatidylinositol. (1998) (0)
A Palladium Catalyzed Route to a Benzofuran Analogue of Indolactam V ( ILV): Effects on PKC Isotype Selectivity. (1995) (0)
Huperzine A ‐ A Potent Acetylcholinesterase Inhibitor of Use in the Treatment of Alzheimer′s Disease. (1991) (0)
An Examination of π-Facial Selectivity in the Diels-Alder Reaction of a Chiral Diene. (1986) (0)
AN IMPROVED METHOD FOR THE SYNTHESIS OF ANOMERICALLY ALLYLATED C-GLYCOPYRANOSIDES AND C-GLYCOFURANOSIDES (1982) (0)
A PLE-Based Resolution of Cocaine, Pseudococaine, and 6- and 7- Methoxylated Cocaine Analogues. (1996) (0)
Synthesis 2006, 2, 243 (2006) (0)
Synthesis of N(1)-substituted analogues of (2R,4R)-4-amino-pyrrolidine-2,4-dicarboxylic acid as agonists, partial agonists, and antagonists of group II metabotropic glutamate receptors. (2001) (0)
A Total Synthesis of Actinobolin via the Intermolecular Diels-Alder Reaction of a Threonine Derived Diene. (1987) (0)
Synthesis of Novel Metabolically Stable Analogues of D‐myo‐Inositol 1, 4,5‐Trisphosphate. (1996) (0)
BOROHYDRIDE INDUCED CLEAVAGE OF AZO DERIVATIVES OF β-KETOESTERS. A USEFUL VARIANT OF THE JAPP-KLINGEMANN REACTION FOR C-NUCLEOSIDE SYNTHESIS (1978) (0)
Abstract 3287: Targeting GSK-3: a new approach for the treatment of neuroblastoma (2015) (0)
Synthesis of Streptazolin (I): Use of the Aza-Ferrier Reaction in Conjunction with the INOC Process to Deliver a Unique but Sensitive Natural Product. (1991) (0)
Abstract 3078: GSK-3 inhibitor 9ING41 potentiates the antitumor effects of CPT-11 in human breast cancer (2016) (0)
Abstract LB-294:In vivoevaluation of Ames negative HDAC6 inhibitor in melanoma model (2017) (0)
Synthesis of Methoxy and Hydroxy Analogues of 1,2,3,4,4a,9a-Hexahydro-4a-fluorenamine: Rigid Phencyclidine Analogues as Probes of Phencyclidine Binding Site Topography. (1991) (0)
Tools for Cell Signaling: Synthesis of the 3-Phosphatase-Resistant 1,3, 4,5-InsP4 Mimic, 1D-myo-Inositol 1,4,5-Trisphosphate 3- Phosphorothioate. (1994) (0)
Life and Death Decisions: Medicinal Chemistry Approaches to Apoptosis (1998) (0)
Location, Location, Location (2011) (0)
The INOC Approach to the Hydroazulenone Ring System. A Potential Entry to the Guaianolides and Pseudoguaianolides. (1983) (0)
A Convenient Method for the Synthesis of Unsymmetrical 3,4‐ Disubstituted Pyrroles. (1992) (0)
Synthesis of the Thiazolone Analogue of the Acetylcholinesterase Inhibitor, Huperzine A. (1994) (0)
Abstract 4055: Enhancing anti-PD-1 immune blockade in melanoma through selective inhibition of histone deacetylase 6 (2017) (0)
Synthesis of the 6- and 7-Hydroxylated Cocaines and Pseudococaines. (1996) (0)
A tandem Michael addition ring-closure route to the metabotropic receptor ligand alpha-(hydroxymethyl)glutamic acid and its gamma-alkylated derivatives. (2001) (0)
A Biomimetic Route to the Ergot Derailment Products, the Clavicipitic Acids. (1986) (0)
CCDC 151515: Experimental Crystal Structure Determination (2001) (0)
Synthesis and Biological Evaluation of 1‐Azabicyclo[3.2.1]octanes: New Dopamine Transporter Inhibitors. (2000) (0)
N‐Phenylalkyl‐Substituted Tropane Analogues of Boat Conformation with High Selectivity for the Dopamine versus Serotonin Transporter. (2000) (0)
1D-myo-Inositol 1,4,5-Trisphosphate and 1D-myo-Inositol 1,3,4,5- Tetrakisphosphate Analogues Modified at C-3; Synthesis of 1D-3-C-( Trifluoromethyl)-myo-inositol 1,4,5-Trisphosphate and 1L-chiro- Inositol 1,2,3,5-Tetrakisphosphate from L-Quebrachitol. (1994) (0)
THE ROLE OF HISTONE DEACETYLASE 6 (HDAC6) IN MUTANT GLYCYL-TRNA SYNTHETASE (GARS) AND MUTANT SMALL HEAT SHOCK PROTEIN B1 (HSPB1)-INDUCED AXONAL CHARCOT-MARIE-TOOTH DISEASE (CMT) (2016) (0)
11P Novel HDAC6 inhibitors show anti-lymphoma activity alone and in combination with venetoclax and copanlisib (2022) (0)
Total Synthesis of 3‐Chloro‐3‐deoxy‐1‐O‐(1,2‐di‐O‐palmitoyl‐sn‐glycero‐ 3‐phospho)‐D‐myo‐inositol. A Potential Mechanistic Probe for Phosphoinositide Signal Transduction Pathways. (1994) (0)
CCDC 151514: Experimental Crystal Structure Determination (2001) (0)
An Approach to Modified Heterocyclic Analogues of Huperzine A and Isohuperzine A. Synthesis of the Pyrimidone and Pyrazole Analogues, and Their Anticholinesterase Activity. (1996) (0)
Structural Remodeling of Cocaine: Design and Synthesis of Trisubstituted Cyclopropanes as Selective Serotonin Reuptake Inhibitors. (2006) (0)
A NITRILE OXIDE BASED ENTRY TO 2,3-DIHYDROPYRAN-4-ONES. SYNTHESIS OF A PROTECTED VERSION “COMPACTIN LACTONE” IN RACEMIC AND OPTICALLY ACTIVE FORMS (1985) (0)
Erratum: The intramolecular nitrile oxide cycloaddition route to spirocyclic alkaloids. A total synthesis of isonitramine and sibirine (Journal of the Chemical Society, Chemical Communications (1985) (847)) (1985) (0)
Cover Picture: Design, Synthesis, and SAR Studies of Mefloquine-Based Ligands as Potential Antituberculosis Agents (ChemMedChem 6/2006) (2006) (0)
Abstract 1703: The HDAC6 inhibitor Nexturastat A improvesin vivoPD-1 immune blockade (2018) (0)
Synthesis of N-(1-(2-Thienyl)cyclohexyl)piperidine (TCP) Based Irreversible Alkylators of the Phenylcyclidine (PCP) Recognition Site. (1992) (0)
LQ12, A Novel PKC Activator, Enhances sAPP Secretion in PC-12 Cells (1999) (0)
Synthesis of Partial Nonpeptidic Peptide Mimetics as Potential Neurotensin Agonists and Antagonists. (1995) (0)
Synthesis of Optically Active Thiadecalins and Thiahydrindans by a Proline-Catalyzed Intramolecular Michael Reaction. (1989) (0)
Efficient Synthetic Routes to Fluorinated Isosteres of Inositol and Their Effects on Cellular Growth. (1990) (0)
The preclinical candidate indole-2-carboxamide improves immune responses to Mycobacterium tuberculosis infection in healthy subjects and individuals with type 2 diabetes (2019) (0)
Synthesis and Pharmacological Evaluation of Benzofuranacetamides as “Antineophobic” Mitochondrial DBI Receptor Complex Ligands. (1998) (0)
Design, Synthesis, and Biological Evaluation of 7-Azatricyclodecanes: Analogues of Cocaine. (2000) (0)
SYNTHESIS OF THE ′SUPPOSED′ CANNIVONINE: A CONSTITUENT OF NEW BRUNSWICK CRANBERRY LEAVES (1979) (0)
Total Syntheses of (+)-Himbacine (XI) and (+)-Himbeline (IX). (1995) (0)
Synthesis, Molecular Modeling, 2‐D NMR, and Biological Evaluation of ILV Mimics as Potential Modulators of Protein Kinase C. (1993) (0)
Structure of human PDK1 kinase domain in complex with UCN-01 (2004) (0)

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What Schools Are Affiliated With Alan Paul Kozikowski?

Alan Paul Kozikowski is affiliated with the following schools:

University of Milan
University of Messina
Chiba University
University of Alberta
KU Leuven
Georgetown University
University of Bologna
University of Illinois Chicago