Jeffrey Aubé

Q: What Schools Are Affiliated With Jeffrey Aubé

Jeffrey Aubé is affiliated with the following schools: Yale University, University of Regensburg, University of Kansas, North Dakota State University, University of North Carolina at Chapel Hill, University of Miami, Duke University

Jeffrey Aubé's AcademicInfluence.com Rankings

Jeffrey Aubé

Chemistry

#3717

World Rank

#4757

Historical Rank

Organic Chemistry

#583

World Rank

#672

Historical Rank

chemistry Degrees

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Chemistry

Jeffrey Aubé's Degrees

PhD Medicinal Chemistry University of Kansas
Bachelors Chemistry University of Kansas

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Jeffrey Aubé'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

The internal quaternary ammonium receptor site of Shaker potassium channels (1993) (271)
MAIT cells are imprinted by the microbiota in early life and promote tissue repair (2019) (262)
Chemistry of bridged lactams and related heterocycles. (2013) (171)
Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria (2016) (160)
Intramolecular Schmidt Reaction of Alkyl Azides (1991) (155)
Characterization of a Cdc42 Protein Inhibitor and Its Use as a Molecular Probe* (2013) (134)
Intramolecular Schmidt Reactions of Alkyl Azides with Ketones: Scope and Stereochemical Studies (1995) (133)
Development of Functionally Selective, Small Molecule Agonists at Kappa Opioid Receptors* (2013) (123)
Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes (2015) (118)
Identification and validation of novel small molecule disruptors of HuR-mRNA interaction. (2015) (101)
Natural product (−)‐gossypol inhibits colon cancer cell growth by targeting RNA‐binding protein Musashi‐1 (2015) (99)
Tumor suppressor TET2 promotes cancer immunity and immunotherapy efficacy. (2019) (97)
Intramolecular Friedel-Crafts Acylation Reaction Promoted by 1,1,1,3,3,3-Hexafluoro-2-propanol. (2015) (95)
One-Step Conversion of Aldehydes to Oxazolines and 5,6-Dihydro-4H-1,3-oxazines Using 1,2- and 1,3-Azido Alcohols (1996) (90)
Reactions of Alkyl Azides and Ketones as Mediated by Lewis Acids: Schmidt and Mannich Reactions Using Azide Precursors (2000) (89)
A Potent and Selective Inhibitor of Cdc42 GTPase (2010) (86)
Syntheses of the Stemona alkaloids (+/-)-stenine, (+/-)-neostenine, and (+/-)-13-epineostenine using a stereodivergent Diels-Alder/azido-Schmidt reaction. (2008) (82)
A Functional Assay for Quantitation of the Apparent Affinities of Ligands of P-Glycoprotein in Caco-2 Cells (2001) (82)
Hexafluoro-2-propanol-Promoted Intermolecular Friedel-Crafts Acylation Reaction. (2016) (77)
First asymmetric total synthesis of (+)-sparteine. (2002) (77)
Revisiting a classic approach to the Aspidosperma alkaloids: an intramolecular Schmidt reaction mediated synthesis of (+)-aspidospermidine. (2005) (76)
Facile C-N cleavage in a series of bridged lactams. (2005) (75)
Regiocontrol in an intramolecular Schmidt reaction: total synthesis of (+)-aspidospermidine. (2000) (72)
Cation-pi control of regiochemistry of intramolecular schmidt reactions en route to bridged bicyclic lactams. (2007) (70)
A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition. (2012) (69)
Asymmetric Schmidt reaction of hydroxyalkyl azides with ketones. (2003) (69)
Probing Chemical Space with Alkaloid-Inspired Libraries (2014) (66)
Asymmetric total synthesis of dendrobatid alkaloids: preparation of indolizidine 251F and its 3-desmethyl analogue using an intramolecular Schmidt reaction strategy. (2004) (66)
Cyclizations of substituted benzylidene-3-alkenylamines: synthesis of the tricyclic core of the martinellines. (2000) (62)
Optimization of potent hepatitis C virus NS3 helicase inhibitors isolated from the yellow dyes thioflavine S and primuline. (2012) (62)
Medium-bridged lactams: a new class of non-planar amides. (2011) (61)
Drug repurposing and the medicinal chemist. (2012) (61)
Overcoming product inhibition in catalysis of the intramolecular Schmidt reaction. (2013) (58)
A tandem Prins/Schmidt reaction approach to marine alkaloids: formal and total syntheses of lepadiformines A and C. (2010) (57)
HuR-targeted small molecule inhibitor exhibits cytotoxicity towards human lung cancer cells (2017) (57)
Lewis Acid-Mediated Reactions of Alkyl Azides with α,β-Unsaturated Ketones (2003) (56)
Practical Electrochemical Anodic Oxidation of Polycyclic Lactams for Late Stage Functionalization. (2015) (56)
An expeditious total synthesis of (+/-)-stenine. (2005) (55)
An efficient computational model to predict protonation at the amide nitrogen and reactivity along the C-N rotational pathway. (2015) (55)
Synthetic aspects of an asymmetric nitrogen-insertion process: preparation of chiral, non-racemic caprolactams and valerolactams. Total synthesis of (-)-alloyohimbane (1990) (54)
Determination of Structures and Energetics of Small- and Medium-Sized One-Carbon-Bridged Twisted Amides using ab Initio Molecular Orbital Methods: Implications for Amidic Resonance along the C-N Rotational Pathway. (2015) (54)
Oxiziridine rearrangements in asymmetric synthesis (1997) (52)
Stereocontrol in a combined allylic azide rearrangement and intramolecular Schmidt reaction. (2012) (52)
Efficient Nitrogen Ring-Expansion Process Facilitated by in Situ Hemiketal Formation. An Asymmetric Schmidt Reaction (1995) (52)
Highly stereoselective ring expansion reactions mediated by attractive cation-n interactions. (2008) (52)
Diastereotopic group-selective reactions at π-arene chromium derivatives. Deprotonation and nucleophilic addition reactions of substrates bearing benzylic chiral centers (1990) (51)
A new twist on amide solvolysis. (2012) (51)
Symmetry-Driven Synthesis of Indole Alkaloids: Asymmetric Total Syntheses of (+)-Yohimbine, (-)-Yohimbone, (-)-Yohimbane, and (+)-Alloyohimbane (1994) (50)
New copper(I)-catalyzed reactions of oxaziridines: stereochemical control of product distribution (1992) (50)
Regiochemical studies of the ring expansion reactions of hydroxy azides with cyclic ketones. (2000) (49)
Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315. (2013) (48)
Synthesis and evaluation of peptidyl Michael acceptors that inactivate human rhinovirus 3C protease and inhibit virus replication. (1998) (48)
Use of a tandem Prins/Friedel-Crafts reaction in the construction of the indeno-tetrahydropyridine core of the haouamine alkaloids: formal synthesis of (-)-haouamine A. (2011) (48)
Principles of Asymmetric Synthesis (2012) (48)
Structure-activity relationship studies of functionally selective kappa opioid receptor agonists that modulate ERK 1/2 phosphorylation while preserving G protein over βarrestin2 signaling bias. (2015) (47)
Opposing reactions in coenzyme A metabolism sensitize Mycobacterium tuberculosis to enzyme inhibition (2019) (46)
A combined intramolecular Diels-Alder/intramolecular schmidt reaction: formal synthesis of (+/-)-stenine. (2002) (46)
Metarrestin, a perinucleolar compartment inhibitor, effectively suppresses metastasis (2018) (46)
Chemotype-selective Modes of Action of κ-Opioid Receptor Agonists* (2013) (45)
Asymmetric total synthesis of dendrobatid alkaloid 251F. (2002) (44)
TiCl4-mediated reactions of alkyl azides with cyclic ketones (1992) (44)
Targeting the interaction between RNA-binding protein HuR and FOXQ1 suppresses breast cancer invasion and metastasis (2020) (43)
Synthesis of a small library of diketopiperazines as potential inhibitors of calpain. (2005) (43)
Mucosal-associated invariant and γδ T cell subsets respond to initial Mycobacterium tuberculosis infection. (2018) (43)
Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold. (2014) (42)
Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy. (2012) (42)
Remodeling and Enhancing Schmidt Reaction Pathways in Hexafluoroisopropanol. (2016) (42)
Asymmetric deprotonation and complexation reactions mediated by chiral ketals as a route to ortho-disubstituted (η6-arene)Cr(CO)3 complexes (1992) (41)
Discovery, Synthesis, and Optimization of Diarylisoxazole‐3‐carboxamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore (2015) (39)
Development of (E)-2-((1,4-Dimethylpiperazin-2-ylidene)amino)-5-nitro-N-phenylbenzamide, ML336: Novel 2-Amidinophenylbenzamides as Potent Inhibitors of Venezuelan Equine Encephalitis Virus (2014) (38)
Structural characterization of N-protonated amides: regioselective N-activation of medium-bridged twisted lactams. (2010) (38)
Intramolecular and Intermolecular Schmidt Reactions of Alkyl Azides with Aldehydes. (2007) (38)
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis (2016) (37)
Proximity effects in nucleophilic addition reactions to medium-bridged twisted lactams: remarkably stable tetrahedral intermediates. (2010) (37)
Unusual tethering effects in the Schmidt reaction of hydroxyalkyl azides with ketones: cation-pi and steric stabilization of a pseudoaxial phenyl group. (2003) (37)
Intramolecular reactions of benzylic azides with ketones: competition between Schmidt and Mannich pathways. (2001) (36)
Ring expansive routes to quinolizidine alkaloids: formal synthesis of (-)-lasubine II. (2003) (36)
A Concomitant Allylic Azide Rearrangement/Intramolecular Azide–Alkyne Cycloaddition Sequence (2014) (36)
Human antigen R as a therapeutic target in pathological cardiac hypertrophy. (2019) (35)
One-step synthesis of oxazoline and dihydrooxazine libraries. (2007) (35)
Butitaxel analogues: synthesis and structure-activity relationships. (1997) (35)
Activation of HuR downstream of p38 MAPK promotes cardiomyocyte hypertrophy. (2016) (35)
Ring expansion by in situ tethering of hydroxy azides to ketones: The boyer reaction (1997) (34)
Novel cytotoxic 3'-(tert-butyl) 3'-dephenyl analogs of paclitaxel and docetaxel. (1995) (34)
Mechanism of the acid-promoted intramolecular schmidt reaction: theoretical assessment of the importance of lone pair-cation, cation-π, and steric effects in controlling regioselectivity. (2012) (34)
N‐Phenylbenzamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore (2016) (34)
Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine (2019) (34)
Domino reactions that combine an azido-Schmidt ring expansion with the Diels-Alder reaction. (2004) (34)
Metal-catalyzed Cross-coupling Reactions Edited by François Diederich and Peter J. Stang. Wiley−VCH, Weinheim. 1998. xxi + 517 pp. 17 × 25 cm. ISBN 3-527-29421-X. $140.00. (1999) (33)
Transport characteristics of peptides and peptidomimetics: I. N-methylated peptides as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa. (2001) (33)
Rearrangements of bicyclic nitrones to lactams: comparison of photochemical and modified Barton conditions. (2003) (32)
Regiochemistry in the intramolecular cycloadditions of substituted 5-alkenyl and 6-alkenyl nitrones (1985) (32)
Hydrolysis of Iminium Ethers Derived from the Reaction of Ketones with Hydroxy Azides: Synthesis of Macrocyclic Lactams and Lactones (1999) (32)
Investigation of the role of βarrestin2 in kappa opioid receptor modulation in a mouse model of pruritus (2015) (32)
Structural analysis of β-turn mimics containing a substituted 6-aminocaproic acid linker (1995) (32)
Asymmetric synthesis with chiral hydroxylamines. Synthesis of optically pure 4-substituted azetidinones (1987) (32)
A Pan-GTPase Inhibitor as a Molecular Probe (2015) (32)
Remote control of diastereoselectivity in intramolecular reactions of chiral allylsilanes. (2006) (31)
Reactivity toward deamidation of asparagine residues in beta-turn structures. (2000) (30)
Modular Synthesis of Cyclic Peptidomimetics Inspired by γ-Turns† (2005) (30)
The HuR CMLD-2 inhibitor exhibits antitumor effects via MAD2 downregulation in thyroid cancer cells (2019) (30)
Stability of medium-bridged twisted amides in aqueous solutions. (2009) (30)
Base-promoted reactions of bridged ketones and 1,3- and 1,4-haloalkyl azides: competitive alkylation vs azidation reactions of ketone enolates. (2004) (29)
Natural product derivative Gossypolone inhibits Musashi family of RNA-binding proteins (2018) (29)
1,3-allylic strain as a strategic diversification element for constructing libraries of substituted 2-arylpiperidines. (2011) (28)
Seeking (and Finding) Biased Ligands of the Kappa Opioid Receptor. (2017) (28)
G protein signaling–biased agonism at the κ-opioid receptor is maintained in striatal neurons (2018) (28)
Identification of Positive Allosteric Modulators of the D1 Dopamine Receptor That Act at Diverse Binding Sites (2018) (28)
Efficient synthesis of gamma-lactams by a tandem reductive amination/lactamization sequence. (2008) (28)
Directed regiochemical control in the ring expansion reactions of a substituted trans-decalone (1990) (27)
Reagent-controlled regiodivergent ring expansions of steroids (2018) (27)
Synthesis and receptor profiling of Stemona alkaloid analogues reveal a potent class of sigma ligands (2011) (27)
Corey-Chaykovsky epoxidation of twisted amides: synthesis and reactivity of bridged spiro-epoxyamines. (2009) (27)
Asymmetric total synthesis of alkaloids 223A and 6-epi-223A. (2009) (26)
Copper-catalyzed oxaziridine-mediated oxidation of C-H bonds. (2012) (26)
Structural and Functional Evaluation of Clinically Relevant Inhibitors of Steroidogenic Cytochrome P450 17A1 (2017) (26)
In situ generation and intramolecular Schmidt reaction of keto azides in a microwave-assisted flow format. (2011) (26)
Synthesis and rearrangement of a bridged thioamide. (2009) (26)
Modular Synthesis of Triazole-Containing Triaryl α-Helix Mimetics (2011) (26)
Synthesis, stabilization, and characterization of the MR1 ligand precursor 5-amino-6-D-ribitylaminouracil (5-A-RU) (2018) (25)
Intramolecular Schmidt reactions of alkyl azides with ketals and enol ethers (1996) (25)
Double conjugate addition of a nitropropionate ester to a quinone monoketal: synthesis of an advanced intermediate to (+/-)-gelsemine. (2007) (24)
Optimization of Potent and Selective Quinazolinediones: Inhibitors of Respiratory Syncytial Virus That Block RNA-Dependent RNA-Polymerase Complex Activity (2014) (24)
Identification of a small molecule yeast TORC1 inhibitor with a multiplex screen based on flow cytometry. (2012) (24)
Reaction discovery using microfluidic-based multidimensional screening of polycyclic iminium ethers. (2010) (24)
Total synthesis of curacin A (1996) (24)
Oxaziridine-Mediated Ring Expansions of Substituted Cyclobutanones: Synthesis of (-)-γ-Amino-β-Hydroxybutyric Acid (GABOB) (1991) (23)
Syntheses and rearrangements of spirocyclic oxaziridines derived from unsymmetrical ketones (1991) (23)
Nonbonded, attractive cation-pi interactions in azide-mediated asymmetric ring expansion reactions. (2008) (23)
N-Alkyl-octahydroisoquinolin-1-one-8-carboxamides: Selective and Nonbasic κ-Opioid Receptor Ligands (2010) (23)
Synthesis of medium-bridged twisted lactams via cation-pi control of the regiochemistry of the intramolecular Schmidt reaction. (2010) (23)
Application of the intramolecular Schmidt reaction to the asymmetric synthesis of (−)-indolizidine 209B from pulegone (1993) (23)
Regioselective single and double conjugate additions to substituted cyclohexa-2,5-dienone monoacetals. (2005) (22)
Stereoselective Synthesis of Freidinger Lactams Using Oxaziridines Derived from Amino Acids. (1997) (22)
SYNTHESIS OF FUNCTIONALIZED N-ALKYL HETEROCYCLES FROM KETONES BY A SEQUENTIAL RING EXPANSION/NUCLEOPHILIC ADDITION PROCESS (1996) (22)
Direct synthesis of medium-bridged twisted amides via a transannular cyclization strategy. (2009) (22)
Synthesis and conformational studies of dipeptides constrained by disubstituted 3-(aminoethoxy)propionic acid linkers. (2004) (21)
High-Throughput Screening, Discovery, and Optimization To Develop a Benzofuran Class of Hepatitis C Virus Inhibitors. (2015) (21)
Discovery of Sulfonamidebenzamides as Selective Apoptotic CHOP Pathway Activators of the Unfolded Protein Response (2014) (21)
DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites. (2016) (21)
Lewis acid-mediated cyclizations of (2′-amino-N′-tert-butoxycarbonyl-benzylidene)-3-alkenylamines (1998) (21)
Selectivity in an asymmetric nitrogen insertion process (1988) (21)
HFIP in Organic Synthesis. (2022) (21)
A Selective ATP-Binding Cassette Subfamily G Member 2 Efflux Inhibitor Revealed via High-Throughput Flow Cytometry (2013) (20)
Minor withanolides of Physalis longifolia: structure and cytotoxicity. (2013) (20)
Cation-n control of regiochemistry of intramolecular Schmidt reactions en route to bridged bicyclic lactams. (2009) (20)
Solution-Phase Parallel Synthesis of a Library of ? 2 -Pyrazolines (2007) (19)
TOTAL SYNTHESIS OF (+)-CURACIN A, A MARINE CYTOTOXIC AGENT (1997) (19)
Characterization of kappa opioid receptor mediated, dynorphin-stimulated [35S]GTPγS binding in mouse striatum for the evaluation of selective KOR ligands in an endogenous setting (2015) (19)
1,7-Asymmetric induction in a nitrogen ring expansion process facilitated by in situ tethering. (1999) (19)
Synthesis and Cytotoxicity of Semisynthetic Withalongolide A Analogues. (2013) (18)
Explorations of stemona alkaloid-inspired analogues: skeletal modification and functional group diversification. (2008) (18)
Reactions of cyclopropanone acetals with alkyl azides: carbonyl addition versus ring-opening pathways. (2007) (18)
Transport characteristics of peptides and peptidomimetics: II. Hydroxyethylamine bioisostere-containing peptidomimetics as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa. (2001) (18)
Deprotonations, conjugate additions, and enolate trapping of oxime ethers and dimethylhydrazones using KDA : The effect of diisopropylamine on enolate trapping (1980) (17)
Synthesis of α-Amino-α‘-diazomethyl Ketones via Ring Opening of Substituted Cyclopropanones with Alkyl Azides. A Facile Route to N-Substituted 3-Azetidinones (2000) (17)
Nucleophilic addition to iminium ethers in the preparation of functionalized N-alkyl heterocycles. (2008) (17)
Stereodivergent synthesis of enantioenriched 4-hydroxy-2-cyclopentenones. (2014) (17)
Three-component synthesis of 1,4-diazepin-5-ones and the construction of gamma-turn-like peptidomimetic libraries. (2008) (17)
Toward the synthesis of sparteine: Intramolecular Schmidt reactions on a norbornanone platform (1996) (17)
HuR Reduces Radiation-Induced DNA Damage by Enhancing Expression of ARID1A (2019) (17)
The NIH's role in accelerating translational sciences (2012) (17)
Efficient 5-OP-RU-Induced Enrichment of Mucosa-Associated Invariant T Cells in the Murine Lung Does Not Enhance Control of Aerosol Mycobacterium tuberculosis Infection (2020) (17)
ML336: Development of Quinazolinone-Based Inhibitors Against Venezuelan Equine Encephalitis Virus (VEEV) (2013) (16)
Diastereoselectivity in the intramolecular cycloaddition reactions of nitrones derived from 5-alkenals and chiral hydroxylamines (1991) (16)
Synthesis and reactivity of bicyclo[3.2.1]octanoid-derived cyclopropanes. (2011) (16)
Mannich reactions using benzyl azide as a latent N- (phenylamino)methylating agent (1998) (16)
Synthesis, structural analysis, and reactivity of bridged orthoamides by intramolecular Schmidt reaction. (2010) (16)
6.15 Hofmann, Curtius, Schmidt, Lossen, and Related Reactions (2014) (15)
(S)-N-(2,5-Dimethylphenyl)-1-(quinoline-8-ylsulfonyl)pyrrolidine-2-carboxamide as a small molecule inhibitor probe for the study of respiratory syncytial virus infection. (2012) (15)
Automated three-component synthesis of a library of γ-lactams (2012) (15)
A Small Molecule Inhibitor of the MITF Molecular Pathway (2014) (15)
An RNA-Binding Protein, Hu-antigen R, in Pancreatic Cancer Epithelial to Mesenchymal Transition, Metastasis, and Cancer Stem Cells (2020) (15)
Effect of progressive benzyl substitution on the conformations of aminocaproic acid-cyclized dipeptides. (2001) (14)
Structure-Based Design of Inhibitors with Improved Selectivity for Steroidogenic Cytochrome P450 17A1 over Cytochrome P450 21A2. (2018) (14)
Small Molecules Targeting the Mitochondrial Permeability Transition (2015) (14)
Diastereotopic group selectivity in the deprotonation of (η-arene)Cr(CO)3 complexes (1988) (14)
Design, synthesis, and evaluation of azapeptides as substrates and inhibitors for human rhinovirus 3C protease. (1999) (14)
Application of the DP4 Probability Method to Flexible Cyclic Peptides with Multiple Independent Stereocenters: The True Structure of Cyclocinamide A. (2018) (14)
Synthesis of N-alkyl-octahydroisoquinolin-1-one-8-carboxamide libraries using a tandem Diels-Alder/acylation sequence. (2007) (14)
Ab initio approach to understanding the stereoselectivity of reactions between hydroxyalkyl azides and ketones. (2004) (14)
High-Throughput Screening Identifies a Bisphenol Inhibitor of SV40 Large T Antigen ATPase Activity (2012) (14)
One-pot synthesis of lactams using domino reactions: combination of Schmidt reaction with Sakurai and aldol reactions. (2009) (14)
Synthesis of Enantiopure N-tert-Butoxycarbonyl-2-aminocycloalkanones (1992) (14)
ML365: Development of Bis-Amides as Selective Inhibitors of the KCNK3/TASK1 Two Pore Potassium Channel (2013) (14)
An enantioselective synthesis of (−)-alloyohimbane (1988) (13)
Single-Cell Transcriptional Profiling Reveals Signatures of Helper, Effector, and Regulatory MAIT Cells during Homeostasis and Activation (2022) (13)
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle. (2017) (13)
(2S, 3S, 5S)- and (2S, 3S, 5R)-5-carboxaldehyde-2,3-diphenyl-1,4-dioxane as surrogates for optically pure 2,3-O-isopropylideneglyceraldehyde in asymmetric synthesis (1992) (13)
Parallel solid-phase synthesis of diaryltriazoles (2012) (13)
Development of a Selective Chemical Inhibitor for the Two-Pore Potassium Channel, KCNK9 (2013) (13)
A small molecule pan-inhibitor of Ras-superfamily GTPases with high efficacy towards Rab7 (2013) (13)
Identification of Inhibitors of Trypanosoma brucei Hexokinases (2011) (12)
Structure-Activity Investigation of a G Protein-Biased Agonist Reveals Molecular Determinants for Biased Signaling of the D2 Dopamine Receptor (2018) (12)
Synthesis of cis-δ-phenylmethyl-d-proline using a nitrogen-centered radical derived from a chiral oxaziridine (1994) (12)
Studies directed at the synthesis of optically active pretazettine via intramolecular nitrone/alkene cycloaddition reactions (1991) (12)
SHAPE-enabled fragment-based ligand discovery for RNA (2022) (12)
Optimization and Evaluation of Antiparasitic Benzamidobenzoic Acids as Inhibitors of Kinetoplastid Hexokinase 1 (2017) (12)
Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D3 Dopamine Receptor Agonist. (2020) (12)
The Schmidt Reaction (2012) (12)
Subsite Ligand Recognition and Cooperativity in the TPP Riboswitch: Implications for Fragment-Linking in RNA Ligand Discovery. (2022) (11)
Synthesis of 13-epi-Taxol via a Transannular Delivery of a Borohydride Reagent (1995) (11)
Effect of stereochemistry on the transport of Aca-linked beta-turn peptidomimetics across a human intestinal cell line. (1997) (11)
Can they imagine the future? A qualitative study exploring the skills employers seek in pharmaceutical sciences doctoral graduates (2019) (11)
Selective Small Molecule Activator of the Apoptotic Arm of the UPR (2013) (11)
An Interrupted Schmidt Reaction: C-C Bond Formation Arising from Nitrilium Ion Capture. (2018) (11)
Resolution of carboxylic acids using copper(I)-promoted removal of propargylic esters under neutral conditions. (2011) (10)
The first synthesis of a C-9 carbonyl modified baccatin III derivative and its conversion to novel taxol® and taxotere® analogues (1994) (10)
Benzylmorpholine Analogs as Selective Inhibitors of Lung Cytochrome P450 2A13 for the Chemoprevention of Lung Cancer in Tobacco Users (2013) (10)
Improved Schmidt Conversion of Aldehydes to Nitriles Using Azidotrimethylsilane in 1,1,1,3,3,3-Hexafluoro-2-propanol (2015) (9)
Discovery, SAR, and Biological Evaluation of Non-inhibitory Chaperones of Glucocerebrosidase (2013) (9)
Dual-Pharmacophore Pyrithione-Containing Cephalosporins Kill Both Replicating and Nonreplicating Mycobacterium tuberculosis. (2019) (9)
Hexafluoroisopropanol and Acetyl Chloride Promoted Catalytic Hydroarylation with Phenols (2018) (9)
Stereospecific synthesis and ring closure of a racemic actinospectose equivalent: a concise route to the spectinomycin series (1986) (8)
Efficient access to sp3-rich tricyclic amine scaffolds through Diels-Alder reactions of azide-containing silyloxydienes. (2016) (8)
Stereochemistry of the oxidation of imines derived from substituted cyclohexanones: axial vs equatorial attack and evidence for delivery by an adjacent hydroxyl group. (2000) (8)
Hepatitis C Virus NS3 Helicase Inhibitor Discovery (2013) (8)
Target Deconvolution of a Multikinase Inhibitor with Antimetastatic Properties Identifies TAOK3 as a Key Contributor to a Cancer Stem Cell–Like Phenotype (2019) (8)
Identification of β-Lactams Active against Mycobacterium tuberculosis by a Consortium of Pharmaceutical Companies and Academic Institutions (2022) (7)
Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif. (2015) (7)
Synthesis of Kappa Opioid Antagonists Based On Pyrrolo[1,2-α]quinoxalinones Using an N-Arylation/Condensation/Oxidation Reaction Sequence. (2016) (7)
Recent Advances in Peptidomimetics (2000) (7)
Synthetic Routes to Lactam Peptidomimetics (1999) (7)
Discovery and Development of Small Molecules That Reduce PNC Prevalence (2010) (7)
The Family Approach to the Resolution of Racemates (2010) (7)
Intramolecular Schmidt Reactions of Alkyl Azides with Ketones: Scope and Stereochemical Studies. (1996) (7)
Identification of novel small molecule Beclin 1 mimetics activating autophagy (2017) (7)
Stereoselectivity in nucleophilic additions to 3-azidoalkanals. (2011) (7)
ATP-Binding Cassette Sub-Family G Member 2 (2013) (7)
Epoxidation and Related Processes (1991) (7)
Schmidt Rearrangement Reactions with Alkyl Azides (2010) (7)
Synthesis and conformation of Gly-Gly dipeptides constrained with phenylalanine-like aminocaproic acid linkers. (2000) (7)
Conformational Analysis and Structural Elucidation of Spirocyclic Oxaziridines Using NMR, Crystallography, and Molecular Modeling (1995) (6)
Synthesis of the Nonribosomal Peptide Phevalin and Analogs. (2019) (6)
Identification of novel small molecule Beclin 1 mimetics activating autophagy. (2017) (6)
Reactions of Oxazolinium and Dihydrooxazinium Salts Prepared by an Azide Insertion Sequence: pH Control of Product Distribution (1998) (6)
N-Alkyl-octahydroisoquinolin-1-one-8-carboxamides: a Novel Class of Selective, Nonbasic, Nitrogen-Containing κ-Opioid Receptor Ligands. (2010) (6)
Activity-Based Protein Profiling Reveals That Cephalosporins Selectively Active on Non-replicating Mycobacterium tuberculosis Bind Multiple Protein Families and Spare Peptidoglycan Transpeptidases (2020) (6)
Bactericidal Disruption of Magnesium Metallostasis in Mycobacterium tuberculosis Is Counteracted by Mutations in the Metal Ion Transporter CorA (2019) (6)
Efficient Synthesis of γ‐Lactams by a Tandem Reductive Amination/Lactamization Sequence. (2008) (6)
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples. (2016) (6)
Inhibition of RNA-binding protein HuR reduces glomerulosclerosis in experimental nephritis (2020) (6)
Domino Acylation/Diels-Alder Synthesis of N-Alkyl-octahydroisoquinolin-1-one-8-carboxylic Acids under Low-Solvent Conditions. (2015) (6)
A divergent route toward lactam-based dipeptidyl building blocks (1992) (5)
Approaches to Cyclic Peptide β-Turn Mimics (2001) (5)
Inhibitors of the Plasmodium falciparum M18 Aspartyl Aminopeptidase (2014) (5)
Intramolecular Friedel—Crafts Acylation Reaction Promoted by 1,1,1,3,3,3-Hexafluoro-2-propanol. (2016) (5)
Selective, reversible inhibitors of the AAA ATPase p97 (2013) (5)
A Cell Based HTS Approach for the Discovery of New Inhibitors of RSV (2013) (5)
Cyclization of a carbon-centered radical derived from oxaziridine cleavage (2006) (4)
Development of Pyrimidone D1 Dopamine Receptor Positive Allosteric Modulators. (2020) (4)
Small-molecule libraries: naturally inspired oligomers. (2012) (4)
Combinatorial Chemistry and Multiple Parallel Synthesis (2010) (4)
Aryl nitrenium ions from N-alkyl-N-arylamino-diazonium precursors: synthesis and reactivity (2014) (4)
Synthesis of cyclic 1,3-diols as scaffolds for spatially directed libraries. (2016) (4)
One-Step Conversion of Aldehydes to Oxazolines and 5,6-Dihydro-4H-1,3- oxazines Using 1,2- and 1,3-Azido Alcohols. (1996) (4)
Report of the 2014-2016 AACP Research and Graduate Affairs Committee (2016) (4)
Identification of a Series of Quinazolinediones as Potent, Selective, Post-Entry Inhibitors of Human Respiratory Syncytial Virus ( h RSV) via a Cell-Based High Throughput Screen and Chemical Optimization (2013) (4)
Symmetry-Driven Synthesis of Indole Alkaloids: Asymmetric Total Syntheses of (+)-Yohimbine, (-)-Yohimbone, (-)-Yohimbane, and (+)- Alloyohimbane. (1995) (4)
One-pot, regiospecific assembly of (E)-benzamidines from δ- and γ-amino acids via an intramolecular aminoquinazolinone rearrangement. (2016) (4)
3-Substituted Biquinolinium Inhibitors of AraC Family Transcriptional Activator VirF from S. flexneri Obtained Through In Situ Chemical Ionization of 3,4-Disubstituted Dihydroquinolines. (2014) (3)
Temperature dependence of turnover in a Sc(OTf)3-catalyzed intramolecular Schmidt reaction. (2015) (3)
Faculty Opinions recommendation of Discovery and inhibition of an interspecies gut bacterial pathway for Levodopa metabolism. (2019) (3)
Synthesis of enantiomerically enriched (R)-5-tert-butylazepan-2-one using a hydroxyalkyl azide mediated ring-expansion reaction (2008) (3)
Identification of selective inhibitors of cdc2-like kinases 1 and 4 (Clk1, Clk4) (2013) (3)
Synthesis of an N‐Substituted Lactam Using An Intramolecular Schmidt Reaction: Formation of 2,3,11,11a‐Tetrahydro‐1H‐Benzo[d]Pyrrolo[1,2‐a]Azepin‐5(6H)‐One (2007) (3)
Efficient Nitrogen Ring‐Expansion Process Facilitated by in situ Hemiketal Formation. An Asymmetric Schmidt Reaction. (1995) (3)
Hexafluoro‐2‐propanol‐Promoted Intermolecular Friedel—Crafts Acylation Reaction. (2016) (3)
Modular Synthesis of Cyclic Peptidomimetics Inspired by γ-Turns. (2005) (3)
Revisiting the β-Lactams for Tuberculosis Therapy with a Compound-Compound Synthetic Lethality Approach (2019) (3)
Selective KOP Receptor Agonists: Probe 1 & Probe 2 (2010) (3)
Profiling a Selective Probe for RTG Branch of Yeast TORC1 Signaling Pathway (2013) (3)
Faculty Opinions recommendation of Open-Air Alkylation Reactions in Photoredox-Catalyzed DNA-Encoded Library Synthesis. (2019) (3)
Efficient 5-OP-RU-induced enrichment of Mucosal-associated invariant T cells in the murine lung does not enhance control of aerosol Mycobacterium tuberculosis infection (2020) (3)
Discovery and Optimization of Pyrrolopyrimidine Derivatives as Selective Disruptors of the Perinucleolar Compartment, a Marker of Tumor Progression toward Metastasis. (2022) (3)
Intramolecular Schmidt Reactions of Alkyl Azides with Ketals and Enol Ethers. (1996) (2)
Asymmetric Synthesis with Chiral Hydroxylamines. Synthesis of Optically Pure 4‐Substituted Azetidinones. (1987) (2)
Unusual spectroscopic and conformational properties of some spirocyclic oxaziridines (1988) (2)
Domino Acylation/Diels—Alder Synthesis of N‐Alkyl‐octahydroisoquinolin‐1‐one‐8‐carboxylic Acids under Low‐Solvent Conditions. (2015) (2)
Chemistry of Bridged Lactams and Related Heterocycles (2013) (2)
Synthesis and Antibacterial Evaluation of Cephalosporin Isosteres (2019) (2)
Unusual Tethering Effects in the Schmidt Reaction of Hydroxyalkyl Azides with Ketones: Cation—π and Steric Stabilization of a Pseudoaxial Phenyl Group. (2004) (2)
3-(2,6-difluorobenzamido)-5-(4-ethoxyphenyl) thiophene-2-carboxylic acid inhibits E.coli UT189 bacterial capsule biogenesis (2013) (2)
Development of biased agonists at the kappa opioid receptor. (2013) (2)
N-(pyridin-4-yl)benzo[d]thiazole-6-carboxamide inhibits E. coli UT189 bacterial capsule biogenesis (2013) (2)
Ring Expansion by in situ Tethering of Hydroxy Azides to Ketones: The Boyer Reaction. (1998) (2)
AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery (2021) (2)
Synthesis of Functionalized N‐Alkyl Heterocycles from Ketones by a Sequential Ring Expansion/Nucleophilic Addition Process. (1996) (2)
A G Protein‐Biased Ligand of the Kappa Opioid Receptor is Antinociceptive and Antipruritic But Does Not Cause Sedation or Dysphoria (2017) (2)
Discovery and Development of Highly Potent Inhibitors of Mycobacterium tuberculosis Growth In Vitro (2013) (2)
Discovery of sultam-containing small-molecule disruptors of the huntingtin–calmodulin protein–protein interaction (2020) (2)
Selective KOP Receptor Antagonists: Probe 1 (2010) (2)
In Vitro and In Vivo Inhibition of the Mycobacterium tuberculosis Phosphopantetheinyl Transferase PptT by Amidinoureas (2022) (2)
Visualizing an Allosteric Intermediate Using CuAAC Stabilization of an NMR Mixed Labeled Dimer. (2021) (2)
Abstract 2449: Targeting an “undruggable” RNA-binding protein: Discovery of small molecule inhibitors of HuR for novel breast cancer therapy (2015) (1)
Synthesis of Amides by Rearrangement (2006) (1)
Small-Molecule Disruptors of Mutant Huntingtin-Calmodulin Protein-Protein Interaction Attenuate Deleterious Effects of Mutant Huntingtin. (2022) (1)
Characterization of a D1 Dopamine Receptor Positive Allosteric Modulator with a Novel Binding Site (2021) (1)
Medium‐Bridged Lactams: A New Class of Non‐Planar Amides (2011) (1)
Effects of fluorine substitution on substrate conversion by cytochromes P450 17A1 and 21A2. (2021) (1)
Erratum: Characterization of a CDC42 protein inhibitor and its use as a molecular probe (Journal of Biological Chemistry (2013) 288 (8531-8543)) (2014) (1)
Synthesis and structural study of cyclic 5-aminovaleric acid-linked beta-Ala-beta-Ala dipeptides. (2008) (1)
Chapter 3 – Enolate, Azaenolate, and Organolithium Alkylations (2012) (1)
Positive Allosteric Modulators of the D1 Dopamine Receptor Act at Diverse Binding Sites (2018) (1)
The Ex Vivo Treatment of Donor T Cells with Cosalane, an HIV Therapeutic and Small-Molecule Antagonist of CC-Chemokine Receptor 7, Separates Acute Graft-versus-Host Disease from Graft-versus-Leukemia Responses in Murine Hematopoietic Stem Cell Transplantation Models. (2019) (1)
Identification of a small molecule yeast TORC 1 inhibitor with a flow cytometry-based multiplex screen (2012) (1)
Discovery of ML370, an inhibitor of Vibrio cholerae Quorum Sensing Acting via the LuxO response regulator (2014) (1)
Use of AD Informer Set compounds to explore validity of novel targets in Alzheimer's disease pathology (2022) (1)
Faculty Opinions recommendation of Allyl sulfides are privileged substrates in aqueous cross-metathesis: application to site-selective protein modification. (2009) (1)
Stereospecific Synthesis and Ring Closure of a Racemic Actinospectose Equivalent: A Concise Route to the Spectinomycin Series. (1986) (1)
A convenient preparation of 2‐[15N]‐amino‐4,6‐dimethoxypyrimidine (1990) (1)
HuR-dependent expression of Wisp1 is necessary for TGFβ-induced cardiac myofibroblast activity (2022) (1)
Characterization of a Cdc42 protein inhibitor and its use as a molecular probe. (2014) (1)
Enzymatic Synthesis of Diverse Heterocycles by a Noncanonical Nonribosomal Peptide Synthetase. (2021) (1)
Syntheses and Rearrangements of Spirocyclic Oxaziridines Derived from Unsymmetrical Ketones. (1991) (1)
Total Syntheses of Martinella Alkaloids (2003) (1)
Total Synthesis of Curacin A. (1996) (1)
Oxaziridine‐Mediated Ring Expansions of Substituted Cyclobutanones: Synthesis of (‐)‐γ‐Amino‐β‐hydroxybutyric Acid (GABOB). (1991) (1)
Solution-phase parallel synthesis of a library of delta(2)-pyrazolines. (2007) (1)
An Expeditious Total Synthesis of (.+-.)-Stenine. (2006) (1)
Structural and Functional Evaluation of Clinically-Relevant Inhibitors of Steroidogenic Cytochrome P450 17A1 (CYP17A1) (2017) (1)
Inhibitors of the Plasmodium falciparum M17 Leucine Aminopeptidase (2014) (1)
9.01 Enabling Technologies in High Throughput Chemistry (2014) (1)
Single cell transcriptional profiling reveals helper, effector, and regulatory MAIT cell populations enriched during homeostasis and activation (2020) (1)
Correction to "Structure-Activity Relationship Studies of Functionally Selective Kappa Opioid Receptor Agonists that Modulate ERK 1/2 Phosphorylation While Preserving G Protein Over βArrestin2 Signaling Bias". (2017) (1)
Structurally Diverse Positive Allosteric Modulators of the D1 Dopamine Receptor Potentiate G‐Protein and β‐Arrestin‐Mediated Signaling (2016) (1)
Use of a MAIT-Activating Ligand, 5-OP-RU, as a Mucosal Adjuvant in a Murine Model of Vibrio cholerae O1 Vaccination (2022) (1)
Domino Reactions that Combine an Azido‐Schmidt Ring Expansion with the Diels—Alder Reaction. (2005) (1)
Application of the Intramolecular Schmidt Reaction to the Asymmetric Synthesis of (‐)‐Indolizidine 209B from Pulegone. (1993) (1)
Oxaziridine Rearrangements in Asymmetric Synthesis (1998) (1)
(361) A novel G-protein biased kappa opioid that displays analgesic but not dysphoric actions in the rat. (2016) (1)
Figure 4, Stability of Probe ML370 in 1:1 Acetonitrile:PBS (pH 7.4, 23 °C) (2014) (0)
Table 5, Data and liabilities of compounds with reported VEEV activity (2013) (0)
Figure 8, [A: Histogram representing number and...]. (2010) (0)
Table 5, Selected examples of SAR from modifying the phenyl moiety (R2) of the MLS000693334 scaffold (2010) (0)
Figure 12, Clinically relevant small molecules for Gaucher disease (2013) (0)
Table 1, SAR expansion on initial hit SID 85240370 (2013) (0)
Figure 3, Graph depicting stability of the probe to thiol (2013) (0)
Table 5, Probe and Analog Submissions to the MLMR (BioFocus DPI) (2010) (0)
Synthetic Aspects of an Asymmetric Nitrogen-Insertion Process: Preparation of Chiral, Non-Racemic Caprolactams and Valerolactams. Total Synthesis of (-)-Alloyohimbane. (1990) (0)
Figure 1, Structures of small molecules chosen for direct experimental comparison (2013) (0)
Table 3, List of Assays and AIDs for this Project (2013) (0)
Characterization of Novel Biased KOR Agonist‐Mediated Cell Signaling (2016) (0)
Table 2, Solubility of ML370 and Analogs in PBS and LB Media (2014) (0)
Table 2, HTS data for compounds in the benzothiazole chemotype (2013) (0)
Figure 3, Downstream MAP Kinase Activation - Secondary functional assays for KOR agonist probes and selected analogs (2010) (0)
Synthesis, Conformational Analysis, and Biological Activity of Proposed Vitronectin Antagonists (2001) (0)
Natural product derivative Gossypolone inhibits Musashi family of RNA-binding proteins (2018) (0)
Table 3, SAR summary for modification at R2 (2013) (0)
Discovery of sultam-containing small-molecule disruptors of the huntingtin–calmodulin protein–protein interaction (2020) (0)
Figure A6C, LCMS purity data at 214 nm for ML291 1st batch (SID 123083137, CID 52940465); LCMS retention time: 3.074 min; purity at 214 nm = 95.4% (2013) (0)
Table 6, Results of Eurofins Profiling with ML336, Compound: CID60156253 (2013) (0)
Figure 12, Absorbance and fluorescence emission spectra of primuline, thioflavine S, and their individual components (2013) (0)
Table 6, SAR analysis of primuline P2 amide derivatives for NS3 helicase inhibitor discovery (2013) (0)
Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists (2021) (0)
Figure 19, Effect of ML283, CID 50930749, CID 486270, and Telaprevir on Huh7.5 hepatoma cells harboring a stably transfected subgenomic rLuc HCV replicon (2013) (0)
Table 7, Summary of in vitro ADME/T Properties of Kappa Opioid Agonist probe(s) (2010) (0)
Figure 5, Inhibition of Mycobacterium tuberculosis growth by ML242 (2013) (0)
Table 6, Structural Modifications of the Core Region (2014) (0)
Figure 3, Proton NMR spectrum for SID 103904169 (CID 49830258) (2013) (0)
Figure 15, Overlay of dose response curves for probe ML231 (SID 99300522, CID 3392161) (2013) (0)
Figure 7, [(A) The NCI Mechanistic Set...]. (2013) (0)
Figure 10, Structures of representative DNA binding agents (2013) (0)
Figure 8, Regions of the compound hit identified for initial SAR exploration (2013) (0)
Table 1, Assay protocol: The optimized 1536-well protocol (2013) (0)
Figure 4, CID2950007 activity in cell-based GTP-Cdc42 and GTP-Rac1 content G-LISA assays in 3T3 cells stimulated with EGF (2010) (0)
Regiocontrol in an Intramolecular Schmidt Reaction: Total Synthesis of (+)‐Aspidospermidine. (2000) (0)
Table 7, Structural Modifications of the Acyl Group (2014) (0)
Figure 10, Assembly of probe compound ML205, SID 99437306, CID 46931017 (2011) (0)
Figure 9, NCI-60 panel: Dose response growth inhibition curves for ML246 in 60 cancer cell lines (2010) (0)
Figure 7, Efficacy and cytotoxicity analysis of ML333 (2013) (0)
Total Synthesis of (+)-Curacin A, a Marine Cytotoxic Agent. (1998) (0)
Figure 10, High magnification image of translocation experiment in a single cell with with 5 μM ML198 (2013) (0)
Development of Structure‐Activity Relationships for a G protein‐Biased Agonist of the D2 Dopamine Receptor (2015) (0)
[Table, Planned Future Studies]. (2011) (0)
Figure A1, Proton data for SID 99300522 (CID 3392161) (2013) (0)
Figure 2, Chemical stability of ML291, represented by percent of parent remaining over time, in the presence of five-fold molar equivalent of GSH or DTT, incubated at room temperature in 1:1 ACN:PBS, pH 7.4, 1% (v/v) DMSO (2013) (0)
Figure 9, Focus of SAR expansion efforts based on primary efflux data (2013) (0)
[Table, Structure Verification and Purity: 1H NMR, 13C NMR, LCMS and HRMS]. (2011) (0)
Scheme 1, Synthetic route for probe molecule and supporting analogsa (2010) (0)
Table 3, Assays Conducted Using Counter Screening Protocol (2013) (0)
Table 9, Probe Activation of Quorum Sensing in Vibrio cholerae Mutant Strains (2014) (0)
Table 5, Isolated thioflavine S and primuline components for NS3 helicase inhibitor discovery (2013) (0)
Abstract 2863: Dissecting the structural basis for inhibitors of RNA-binding proteins (2018) (0)
Table 7, Comparison of quercetin and probe (2011) (0)
Scheme 1, Synthetic route to ML315 (2013) (0)
Figure 3, General synthetic route to probe ML308 (2013) (0)
Table 5, Assays Conducted Using HepG2 Cell Cytotoxicity Screening Protocol (2013) (0)
Table 5, Receptor Paneling of KOP agonist [ML140] CID3342390 through the PDSP (2010) (0)
Figure 13, Chemical genetic analysis of active compounds on RTG pathway (2013) (0)
Figure 6, HRMS data for SID 103904169 (CID 49830258); HRMS (ESI) m/z calcd for C23H21N6O ([M+H]+), 397.1777, found 397.1776 (2013) (0)
Paying the Pipeliner: Early Stage Drug Discovery in Academica (2006) (0)
Figure 8, Concentration response profiles for probes ML198 and ML266 using 4-methylumbelliferyl-β-D-glucopyranoside (blue) as the substrate, with N370S spleen homogenate (2013) (0)
Selectivity in an Asymmetric Nitrogen Insertion Process. (1988) (0)
Faculty Opinions recommendation of A ring expansion strategy towards diverse azaheterocycles. (2021) (0)
Table 5, SAR summary for modification of the amidoaryl component (2011) (0)
Figure 4, Dose-response curves of ML282 (CID 1067700) with different GTPases (2013) (0)
Table A5, Critical reagents for the E. coli SSB DNA binding assay (2013) (0)
Table 6, Receptor Paneling of KOP agonist Probes 1 [ML139] CID5236771 & 2 [ML138] CID44601470 through the PDSP (Bryan Roth, PI) (2010) (0)
Erratum: Synthesis and receptor profiling of Stemona alkaloid analogues reveal a potent class of sigma ligands (Proceedings of the National Academy of Sciences of the United States of America (2011) 108, 17, (6727-6732) DOI: 10.1073/pnas.1016558108) (2012) (0)
Figure 8, General synthetic route for probe and analogue synthesis (2011) (0)
2‐(t‐Butoxycarbonyloxyimino)‐2‐phenylacetonitrile (2001) (0)
Figure 24, Spectra of CID 50930730/ML283 and some analogues (2013) (0)
Abstract P5-05-09: Chemo-sensitization of triple negative breast cancer by targeting RNA-binding protein HuR (2020) (0)
Scheme 1, Synthesis of Probe ML370 (2014) (0)
Figure B1, Proton NMR spectrum for SID 114279600 (CID 50930730) (2013) (0)
[Table, SUPPLIERS, VENDORS AND CONTACT INFORMATION]. (2010) (0)
Table 4, ADME profile for ML198 and ML266 (2013) (0)
Figure 1, The Endogenous Ligand of the Vibrio cholerae Sensor Histidine Kinase CqsS, Cholera autoinducer-1 (CAI-1) (2014) (0)
Table 3, SAR Analysis for Selective κ–opioid receptor agonist for the Bisamide Scaffold (2010) (0)
Figure 3, CID2950007 Inhibits Cdc42 association with PAK-PBD (2010) (0)
Figure 3, Synthetic scheme for preparation of ML336 (2013) (0)
Lewis Acid Mediated Reactions of Alkyl Azides with α,β-Unsaturated Ketones. (2004) (0)
Figure 13, Representative non imino sugar chaperone inhibitors discovered at the NIH Chemical Genomics Center (2013) (0)
Table 4, Caspase 3/7 activation in response to p97 inhibition assay (2013) (0)
Figure 10, TORC1 bypass cell growth analysis on the probe ML231 and SID 96099781 (2013) (0)
Figure A6D, HRMS data for ML291 1st batch (SID 123083137, CID 52940465); HRMS m/z calculated for C16H17ClN3O6S [M + H+]: 414.0521, found 414.0527 (2013) (0)
Figure 2, Aqueous stability of compound ML231 (SID 99300522, CID 3392161) (2013) (0)
Table 2, Critical reagents for the p97 ATPase dose response assay (2013) (0)
Intramolecular Schmidt Reaction of Alkyl Azides. (1992) (0)
Figure 2, Graph depicting stability of ML282 after 48 h in PBS (no additives) (2013) (0)
Figure A6F, LCMS purity data at 214 nM for ML336, SID 144087340, CID 71301451 (2013) (0)
Table 1, Inhibitors of NS3 helicase known at the time of grant award (2013) (0)
Figure 1, Chemical stability of ML336 over 8 h in the presence of a 5-fold concentration of dithiothreitol (2013) (0)
Modular Synthesis of Triazole-Containing Triaryl α-Helix Mimetics. (2011) (0)
Table 1, Listing of all Assays and AIDs for this project (2010) (0)
Figure 7, Structures of C7 and ML317 (2013) (0)
Identification of a novel, highly potent D3 dopamine receptor‐selective agonist (662.8) (2014) (0)
Synthesis of Enantiopure N‐tert‐Butoxycarbonyl‐2‐aminocycloalkanones. (1993) (0)
Targeting the interaction between RNA-binding protein HuR and FOXQ1 suppresses breast cancer invasion and metastasis (2020) (0)
Abstract 4817: Molecular cancer therapy targeting RNA-binding protein Musashi-1 (2016) (0)
Figure 14, [A. probe structure; B. dose...]. (2011) (0)
Table 4, Second round of SAR study on synthesized analogues (2013) (0)
DEPROTONATIONS, CONJUGATE ADDITIONS, AND ENOLATE TRAPPING OF OXIME ETHERS AND DIMETHYLHYDRAZONES USING POTASSIUM DIISOPROPYLAMIDE. THE EFFECT OF DIISOPROPYLAMINE ON ENOLATE TRAPPING (1980) (0)
Table 5, PubChem Assays Reporting Dose-Dependent Activity of CID 665390 (the hit compound)* (2014) (0)
Chapter 5 – Aldol and Michael Additions of Allyls, Enolates, and Enolate Equivalents (2012) (0)
Table 2, Continuation of SAR expansion on initial hit SID 85240370 (2013) (0)
Figure 12, Refinement of structure based on efflux and associated potentiation and toxicity data (2013) (0)
Table 2, Summary of assays, listed by title and AID, used for the development of ML336* (2013) (0)
Table 4, Probe and analogue submissions to MLSMR (BioFocus DPI) for NS3 helicase inhibitor discovery (2013) (0)
Reversal chemotherapeutic resistance of triple‐negative breast cancer via functionally inhibiting RNA‐binding protein HuR (2022) (0)
Figure 9, Selected compounds for GLISA analysis (AID-2375) (2010) (0)
Abstract P4-01-16: Overcome chemoresistance of triple-negative breast cancer by inhibiting the RNA-binding protein HuR (2022) (0)
[Table, High Content Assay for PNC Detection]. (2010) (0)
Arthur Suite V. 3.0 Symyx Technologies, Inc., 3100 Central Expressway, Santa Clara, CA 95051. www. symyx.com. See Web site for pricing information. (2006) (0)
Figure 5, Schematic drawing of the MBHA mechanism (2013) (0)
Table 7, Properties Computed from Structure CID3342390 (MLS0026993322) (2010) (0)
Development of functionally selective agonists at the kappa opioid receptor (KOR) (2013) (0)
Figure 1, Currently available marketed drugs for treatment of human African trypanosomiasis (2011) (0)
Correction to "Dual-Pharmacophore Pyrithione-Containing Cephalosporins Kill Both Replicating and Nonreplicating Mycobacterium tuberculosis". (2019) (0)
Figure 27, Dose response curves for helicase inhibitors used for comparison (2013) (0)
Table 5, Summary of modifications for R4 (2013) (0)
A Divergent Route Toward Lactam-Based Dipeptidyl Building Blocks. (1994) (0)
Table 7, Probe and analog submissions to MLSMR (BioFocus DPI) for inhibitors of M. tb in 7H9 media (2013) (0)
Hydrolysis of Iminium Ethers Derived from the Reaction of Ketones with Hydroxy Azides: Synthesis of Macrocyclic Lactams and Lactones. (1999) (0)
Abstract PS16-20: Targeting the RNA-binding protein HuR to overcome chemoresistance in triple-negative breast cancer (2021) (0)
Figure 1, Graph depicting stability of ML308 after 48 h in PBS and with PBS/ACN (2013) (0)
Figure 4, Cellular Efficacy of ML291 for Activating the CHOP Pathway Induced cytotoxicity in MEF with wt-CHOP vs. CHOP-KO (2013) (0)
Table 6, Percent of activity remaining for various kinases when inhibited by ML231 (2013) (0)
Lewis acid-mediated reactions of alkyl azides with alpha,beta-unsaturated ketones. (2003) (0)
Table 9, Summary of in vitro ADMET/T Properties for p97ATPase probe(s) (2013) (0)
[Table, Experimental Results]. (2013) (0)
Table 9, SAR analysis of selected fully synthetic analogues for NS3 helicase inhibitor discovery (2013) (0)
Table A3, Critical reagents for the ATP hydrolysis assays (2013) (0)
[Table, Summary of Significant Results]. (2013) (0)
Studies in Natural Products Chemistry: Vol. 16, Stereoselective Synthesis (Part J) Edited by A.-u.-Raman (University of Karachi, Pakistan). Elsevier: The Netherlands. 1995. xiv + 757 pp. $435.25. ISBN 0-444082264-X. (1996) (0)
Table 1, Probe ML282 Assay Data Summary (2013) (0)
Figure 2, Chemical stability of ML308 over 8 h in the presence of 5-fold glutathione or dithiothreitol (2013) (0)
Figure 9, Five analogues selected for submission to support probe ML205, SID 99437306, CID 46931017 and associated data (2011) (0)
Figure 4.1.1, Structures for Compounds Reported to inhibit the mtPTP (2015) (0)
HuR inhibition reduces post-ischemic cardiac remodeling by dampening acute inflammatory gene expression and the innate immune response (2023) (0)
Table 4, Summary of data from primary assay collected on hit compound CID 2950007/MLS000693334 (2010) (0)
Synthetic probes for the study of biological function (2013) (0)
Faculty Opinions recommendation of Asymmetric synthesis of synthetic alkaloids by a tandem biocatalysis/Ugi/Pictet-Spengler-type cyclization sequence. (2010) (0)
Synthesis of cis-δ-Phenylmethyl-D-proline Using a Nitrogen- Centered Radical Derived from a Chiral Oxaziridine. (2010) (0)
Table 3, SAR summary for substitution on the benzoic acid moiety (2011) (0)
Figure 6, Efficacy and cytotoxicity analysis of ML317 (2013) (0)
Figure 5, CID 2950007 inhibits bradykinin-induced filopodia formation (2010) (0)
Table A6, Critical reagents for the HCV subgenomic replicon assay (2013) (0)
Abstract 5162: Id1 is an oncogenic target of RNA binding protein HuR in gastric cancer (2016) (0)
TiCl4-Mediated Reactions of Alkyl Azides with Cyclic Ketones. (1992) (0)
Table 4, Assays Conducted Using Vero Cell Cytotoxicity Screening Protocol (2013) (0)
Table 4, Profiling of the probe, ML246, in the PDSP comprehensive panel (2010) (0)
Abstract 5427: Small molecule inhibitors of Musashi family of RNA-binding proteins (2015) (0)
Table 10, Comparison of known inhibitors of p97ATPase with DBeQ, CID 49830258 [ML240], and CID 49830260 [ML241] (2013) (0)
Figure 25, Effect of compounds on the polarization of a Cy5-dT15-E. coli single-stranded DNA binding protein (SSB) complex (2013) (0)
Figure 3, General synthetic route for preparing probe compound SID 114279600 (CID 50930730) and associated analogues (2013) (0)
Figure 20, Effect of ML283, CID 50930749, and interferon on cellular HCV RNA levels (2013) (0)
In situ Generation and Intramolecular Schmidt Reaction of Keto Azides in a Microwave‐Assisted Flow Format. (2012) (0)
Table 2, Assays Conducted Using Primary Assay Protocol (2013) (0)
Table 2, Solubility for ML282 in Assay Media (2013) (0)
Figure 1, PTB-GFP PC-3M cells (2010) (0)
Abstract 1145: Overcoming chemoresistance and blocking metastasis in breast cancer by targeting HuR (2017) (0)
Figure 4, Stability of ML198 in D-PBS pH 7.4 at room temperature over 48 hr (2013) (0)
Table 5, IC50 values (nM) against Clk and Dyrk kinases for quinazoline and pyrimidine chemotypes (2013) (0)
Table 8, Summary of in vitro ADME/T Properties for probe ML242 (2013) (0)
Figure 5, Five analogues chosen to support probe ML333 (2013) (0)
Figure 7, Validated hit resulting from the preliminary commercial SAR effort (2013) (0)
Table 2, Assessment of CID2950007 in Key Biological Assays (based on CPDP Flow Chart) (2010) (0)
Figure 16, Structures of derivatives based on the major components in primuline (2013) (0)
Figure 15, SAR enhancement of SID 97301789 (2013) (0)
Faculty Opinions recommendation of On the Practical Limits of Determining Isolated Product Yields and Ratios of Stereoisomers: Reflections, Analysis, and Redemption. (2011) (0)
Table 7, Results of Eurofins Profiling with ML336, Compound: CID60156253 continued (2013) (0)
Figure 6, Hit scaffold and dose response curves illustrating selectivity for Cdc42 (2010) (0)
The HuR CMLD-2 inhibitor exhibits antitumor effects via MAD2 downregulation in thyroid cancer cells (2019) (0)
Figure 15, Fused amide analogs and associated data (2011) (0)
Effect of C-2 substitution on the stability of non-traditional cephalosporins in mouse plasma (2019) (0)
Toward the Synthesis of Sparteine: Intramolecular Schmidt Reactions on a Norbornanone Platform. (1996) (0)
Virtual Special Issue: New Drug Modalities in Medicinal Chemistry, Pharmacology, and Translational Science. (2023) (0)
Figure 8, Primary dose response assay data for CID 44216842 (2010) (0)
[Figure], Critical Path Flowchart for KOR Antagonist Project (2010) (0)
Table 2, Supporting analogs with IC50 values (nM) against Clk and Dyrk kinases (2013) (0)
Figure 7, [A) Brief outline of BellBrook...]. (2010) (0)
Table 1, ML336 Data Summary (2013) (0)
Table 3, First round of SAR study on synthesized analogues (2013) (0)
Table 8, Calculated physical properties of Kappa opioid Agonist probe(s) (2010) (0)
Figure 21, Effect of CID 50930749 on the cellular location of HCV Replication complexes seen in the replicon-containing Huh7.5/Con1sg-Rluc cells (2013) (0)
Table 7, Summary of in vitro ADME properties of ML333 (2013) (0)
Table 3, BellBrook Labs Proliferation and Migration Data for Key Compounds (2010) (0)
Synthesis of alpha-amino-alpha'-diazomethyl ketones via ring opening of substituted cyclopropanones with alkyl azides. A facile route to N-substituted 3-azetidinones. (2000) (0)
Figure 4, Structures for which VEEV activity is reported (2013) (0)
Figure 2, Stability studies for ML315 in aqueous PBS (circles) and 50:50 aqueous PBS:acetonitrile (triangles) (2013) (0)
N‐(tert‐Butoxycarbonyloxy)phthalimide (2001) (0)
Scheme 1, [Reagents: (a) substituted benzoyl chloride,...]. (2013) (0)
Figure 1, Summary of the hit structures for the KOP antagonist project (2010) (0)
Figure 2, Aqueous stability of ML336 over 48 h in PBS or PBS/acetonitrile (2013) (0)
Scheme 2, Synthetic route to oxygenated analogues (2013) (0)
Figure 5, Five thiophene analogues chosen to support of probe ML317 (2013) (0)
Figure 7, Stability of ML266 in D-PBS pH 7.4 buffer at room temperature over 48 hr (2013) (0)
Aryl Nitrenium Ions from N‐Alkyl‐N‐arylamino‐diazonium Precursors: Synthesis and Reactivity. (2014) (0)
Table 4, SAR summary for modification of the nitro group at R3 (2013) (0)
Erratum to: Use of a MAIT-Activating Ligand, 5-OP-RU, as a Mucosal Adjuvant in a Murine Model of Vibrio cholerae O1 Vaccination (2022) (0)
Table 6, Probe ML240 and analog submissions to MLSMR (BioFocus DPI) for reversible inhibitors of p97 (2013) (0)
Figure 2, Structure Verification (2013) (0)
Table A8, Critical reagents for the Cellular HCV RNA quantification assay (2013) (0)
Figure 7, Stability data depicted as a graph showing the loss of ML205 with time over a 48 hr period (2011) (0)
Advances in Sulfonamide Kappa Opioid Receptor Antagonists: Structural Refinement and Evaluation of CNS Clearance. (2022) (0)
Table 3, Summary of modifications for R1 (2013) (0)
Figure 2, CID2950007 is a Non-Competitive Inhibitor of Cdc42 (2010) (0)
Modular synthesis of cyclic peptidomimetics inspired by gamma-turns. (2005) (0)
Figure 3, Aqueous stability of compound SID 88095709 (CID 44640177) in PBS and no acetonitrile (closed circles), and aqueous stability of compound SID 88095709 (CID 44640177) in PBS with the addition of acetonitrile (50% v/v final, closed triangles) (2013) (0)
Discovery and characterization of a G protein‐biased agonist of the D2 dopamine receptor (662.7) (2014) (0)
Principles and Applications of Asymmetric Synthesis By Guo-Qiang Lin, Yue-Ming Li, and Albert S. C. Chan. Wiley Interscience, New York. 2001. xvii + 515 pp. 16 × 24 cm. ISBN 0-471-40027-0. $89.95. (2001) (0)
Table 8, Comparison of New & Existing Cholera QS Probes to Project Criteria (2014) (0)
Table 5, In vitro ADME data for ML246 (2010) (0)
Figure 9, Effects primuline and its components on HCV helicase catalyzed DNA unwinding (2013) (0)
Figure 9, Possible Directions for Future SAR Investigation of ML370 (2014) (0)
A Tandem Prins/Schmidt Reaction Approach to Marine Alkaloids: Formal and Total Syntheses of Lepadiformines A (XVI) and C (XVII). (2010) (0)
Abstract 1413: Targeting the RNA-binding protein HuR to overcome chemoresistance in triple-negative breast cancer (2021) (0)
Table 3, CID 2950007 Inhibits Filopodia Formation in 3T3 Fibroblasts (2010) (0)
Table 6, Survey of combined effects of optimized functionality (2011) (0)
[Table, ATP Quantitation Assay (viability assay)]. (2010) (0)
Asymmetric Deprotonation and Complexation Reactions Mediated by Chiral Ketals as a Route to Ortho-Disubstituted (η6-Arene)Cr(CO)3 Complexes. (1992) (0)
Table 1, Comparison of data obtained with variable quercetin sources (2011) (0)
Table 9, Data for marketed and select literature antitubercular drugs in assays used in this report (2013) (0)
Figure 18, P2 and amide derivative substructures used in SciFinder searches (2013) (0)
Figure A6A, 1H NMR spectrum for ML336, SID 152199106, CID 71301451 (2013) (0)
Table 1, Five probe analogues with screening data (2013) (0)
Effect of C-2 substitution on the stability of non-traditional cephalosporins in mouse plasma (2019) (0)
Table 3, Summary of in vitro ADME Properties of UPR CHOP Activator probe ML291 (2013) (0)
Figure 3, Aza-uracil-derived antagonists of LuxO ATPase activity (2014) (0)
Figure 3, Activation of luciferase reporters driven by UPR sub-pathway promoters for the apoptotic (CHOP) and adaptive (XBP1) arms (2013) (0)
Table 5, Comparison of probe to prior art (2013) (0)
Special Section on The Opioid Crisis Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine s (2019) (0)
Table 2, Summary of modifications to R1 (2013) (0)
Table A9, Critical reagents for the Indirect immunofluorescence staining assay (2013) (0)
Small Molecules Targeting the RNA-Binding Protein HuR Inhibit Tumor Growth in Xenografts. (2023) (0)
Figure 13, Effects of thioflavine S and the most potent primuline component on HCV helicase catalyzed ATP hydrolysis (2013) (0)
Table 12, Activity of reference inhibitors under comparison assays (2013) (0)
Figure 14, General synthetic route for preparing probe compound SID 103904185 (CID 49830260) and associated analogues (2013) (0)
Figure 4, General synthetic route for probe and associated analogues (2013) (0)
A novel Mucosal Associated (semi)-invariant T cell (MAIT) activation assay with synthetic MR1 ligand (2016) (0)
The π‐Arene Chromium Complex as a Facial Selectivity Control Element: The Enantioselective Synthesis of Cetirizine Hydrochloride (1997) (0)
Figure A6E, High resolution MS for ML336, SID 144087340, CID 71301451 (2013) (0)
Table 4, Probe and analog submission for Kappa Opioid Antagonists (2010) (0)
The first total synthesis of (-)-FR901483 (1999) (0)
Table 1, Summary of Key Properties for ML246 (2010) (0)
A Cdc42 GTPase Specific Inhibitor as a Molecular Probe and Prototype for Drug Development (2013) (0)
Figure 17, Michaelis-Menten and Lineweaver-Burk plots showing mixed inhibition of TbHK1 with respect to ATP using ML205, SID 99437306, CID 46931017 (2011) (0)
Figure A4, HRMS data for SID 88095709 (CID 44640177) (2013) (0)
Figure 1, Dose Response for CID2950007 against GTPase family members (2010) (0)
Reactions of Oxazolinium and Dihydrooxazinium Salts Prepared by an Azide Insertion Sequence: pH Control of Product Distribution. (1999) (0)
Synthesis of Medium-Bridged Twisted Lactams via Cation– π Control of Regiochemistry of Intramolecular Schmidt Reaction (2010) (0)
Small Molecule Inhibitors of Trypanosoma brucei Hexokinase 1 (2011) (0)
Figure 6, Schematic of screen strategy (2013) (0)
Figure 8, Structure and literature and MLPCN determined potency and selectivity data for C23 (2013) (0)
Abstract 1780: Functional inhibition of RNA-binding protein HuR reverses chemotherapeutic resistance in triple-negative breast cancer (2022) (0)
Abstract B36: Preclinical development of a multikinase targeting molecule with activity against the cancer stem cell phenotype in pancreatic adenocarcinoma (2016) (0)
Table 2, Targets from Ricerca profiling that showed > 50% inhibition (2013) (0)
Figure 5, Dose Response Curves for initial hit (CID 665390) and optimized probe (CID 70680248) (2014) (0)
Figure 1, Ribavarin (2013) (0)
Figure A3, LCMS purity data at 215 nm for SID 88095709 (CID 44640177) (2013) (0)
Figure B4, HRMS data for SID 114279600 (CID 50930730); HRMS (ESI) m/z calcd for C28H19ClN3O4S3 ([M+H]+), 592.0226, found 592.0228 (2013) (0)
The First Synthesis of a C‐9 Carbonyl Modified Baccatin III Derivative and Its Conversion to Novel Taxol and Taxotere Analogues. (1995) (0)
Table A4, Critical reagents for the NS3 protease assay (2013) (0)
Abstract 1753: Functional inhibition of the RNA-binding protein HuR sensitizes triple-negative breast cancer to chemotherapy (2023) (0)
Figure 17, Summary of the SAR strategy to synthesize analogues based on the hit, P3 (2013) (0)
Characterization of the kappa opioid receptor‐mediated G protein signaling in mouse striatum using a [35S]GTPγS binding assay (659.6) (2014) (0)
Cation—π Control of Regiochemistry of Intramolecular Schmidt Reactions en Route to Bridged Bicyclic Lactams. (2007) (0)
Figure 6, Screening flow chart (2013) (0)
Arthur C. Cope Scholar Awards and Eli Lilly Award (2012) (0)
Figure 6, Effect of ML242 (CID 2792221) on three mammalian cell lines (2013) (0)
Figure 8, Dose response analysis of probe compound ML231 (2013) (0)
Synthesis of (±)-Stenine (2006) (0)
Opioid Receptor Agonists κ Chemotype-selective Modes of Action of Signal Transduction : (2013) (0)
Figure A4, HRMS data for SID 99300522 (CID 3392161) (2013) (0)
Figure 6, Compound attrition of the NCI Mechanistic Set library during screening phases (2013) (0)
Figure 11, Sch9 phosphorylation assay on active compounds (2013) (0)
Discovery and Optimization of ML417: A Potent and Highly Selective D3 Dopamine Receptor Agonist (2017) (0)
Synthesis of α‐Amino‐α′‐diazomethyl Ketones via Ring Opening of Substituted Cyclopropanones with Alkyl Azides. A Facile Route to N‐Substituted 3‐Azetidinones. (2000) (0)
Figure A6F, HRMS data for ML291 2nd batch –submitted to the MLSMR (SID 134228465, CID 52940465); HRMS m/z calculated for C16H17ClN3O6S [M + H+]: 414.0521, found 414.0522 (2013) (0)
Figure A1A, Proton data for ML275, SID 124756536, CID 53301904 (2013) (0)
Table 4, SAR summary for substitution of the amide linker region (2011) (0)
Table 6, Fourth round of synthetic analogues (2013) (0)
Figure 10, Parent hit SID 85240370 modified to a new lead, SID 88095709 (2013) (0)
Abstract IA04: Targeting RAS for anticancer therapy (2020) (0)
New Copper(I)‐Catalyzed Reactions of Oxaziridines: Stereochemical Control of Product Distribution. (1992) (0)
Table 3, Protocol of fibroblast translocation experiment (2013) (0)
Chapter 12 The total synthesis of amphibian alkaloids using the intramolecular schmidt reaction (2008) (0)
Figure 2, Known TbHK1 inhibitors and preliminary associated data (2011) (0)
Table D1, Description of the outcome for the screen of 827 compounds from the NCI DTP compound collection (2013) (0)
Figure 10, General synthetic scheme for the synthesis of dihydropyrazolines (2010) (0)
[Table], User Chromatogram Peak List (2011) (0)
Figure 14, Map of the computed solubility of selected compounds in the PLS principal component space (2013) (0)
Table 4, Summary of Probe Properties Computed for ML370 (2014) (0)
Generation of the AD Informer Set: Chemical tools to facilitate Alzheimer’s disease drug discovery (2021) (0)
Figure 9, Structures and select properties for C7, ML317, and ML333 (2013) (0)
Figure 7, Proton NMR spectrum for SID 103904185 (CID 49830260) (2013) (0)
Erratum: Syntheses and rearrangements of spirocyclic oxaziridines derived from unsymmetrical ketones (Journal of Organic Chemistry (1991) 56, (502)) (1991) (0)
(2S,3S,5S)- and (2S,3S,5R)-5-Carboxaldehyde-2,3-diphenyl-1,4-dioxane as Surrogates for Optically Pure 2,3-O-Isopropylideneglyceraldehyde in Asymmetric Synthesis. (1993) (0)
Comparative Pharmacology and Structure–Activity Relationships of D1 Dopamine Receptor Positive Allosteric Modulators (2019) (0)
Table 8, Comparison of prior art and current probe (2010) (0)
Figure 2, The V cholerae CqsS/CAI-1 Quorum Sensing Phosphorelay system (2014) (0)
Faculty Opinions recommendation of Diastereoselective synthesis of gamma-lactams by a one-pot, four-component reaction. (2007) (0)
Table A2, Critical reagents for the DNA binding assays (2013) (0)
Syntheses and rearrangements of spirocyclic oxaziridines derived from unsymmetrical ketones [Erratum to document cited in CA114(9):81656r] (1991) (0)
Table 8, Percent of activity remaining for various kinases when inhibited by SID 88095709 (2013) (0)
Table 1, Percent remaining of ML308 at the conclusion of the experiment (8h) (2013) (0)
Figure 13, Quantitative comparison of prior art to SID 88095709 (2013) (0)
Scheme 1, [Probe Preparation]. (2013) (0)
Figure 7, Characterization of CID 3528206 (SID 96099781) as a TORC1 specific inhibitor (2013) (0)
Figure 12, [A: plot of percent inhibition...]. (2011) (0)
Faculty Opinions recommendation of Synthesis and Explosion Hazards of 4-Azido-l-phenylalanine. (2018) (0)
[Table, Probe Structure and Characteristics]. (2013) (0)
Figure 8, Structures of the isolated components of thioflavine S (T) and primuline (P) (2013) (0)
HuR-targeted small molecule inhibitor exhibits cytotoxicity towards human lung cancer cells (2017) (0)
Table 7, SAR analysis of additional P2 derivatives for NS3 helicase inhibitor discovery (2013) (0)
Table 1, Strains of V. cholera used in assays (2014) (0)
Table 1, Five probe analogues submitted to the NIH MLSMR, and their associated screening data (2013) (0)
[Table, Profiling Assays]. (2011) (0)
Reagent-controlled regiodivergent ring expansions of steroids (2018) (0)
Table 6, Selected examples of SAR from modifying the 4-methoxyphenyl moiety (R3) of the MLS000693334 scaffold (2010) (0)
Figure 3, Graph depicting thiol stability of probe (2013) (0)
Mutant Huntingtin‐Calmodulin Interaction: Potential Therapeutic Target for Huntington's Disease (2019) (0)
Figure 11, Effect of R3 alkyl substitution (2013) (0)
Directed Regiochemical Control in Ring Expansion Reactions of a Substituted trans-Decalone. (1991) (0)
Table 6, Assays Conducted Using THP-1 Cell Cytotoxicity Screening Protocol (2013) (0)
Table 7, Analogues with R1 – R4 substitution patterns in combination (2013) (0)
[Table, PC3M Caspase 3/7 Activation Assay]. (2010) (0)
Table A1, Critical reagents for the helicase assays (2013) (0)
Table 2, Inhibitors of NS3 helicase disclosed since the time of grant award (2013) (0)
Figure 14, RapaGFP clone screening (2013) (0)
Oxaziridines as N- and O-Functionalization Reagents (2000) (0)
CuAAC stabilization of an NMR mixed labeled dimer (2021) (0)
Figure A6E, LCMS purity data at 214 nm for ML291 2nd batch –submitted to the MLSMR (SID 134228465, CID 52940465); LCMS retention time: 3.125 min; purity at 214 nm = 97.5% (2013) (0)
Table 2, Typical protocol of primary and secondary assays (2013) (0)
Scheme 3, Synthetic route to indazole analogues (2013) (0)
Enhancing Mucosal-Associated Invariant T Cell Function and Expansion with Human Selective Serum (2022) (0)
Figure 8, Summary of analogs prepared to investigate the SAR profile of hit CID 665390 (2014) (0)
Table 3A, SAR Analysis for Selective κ –opioid receptor antagonists of the sulfonamide sub-scaffold 1 (2010) (0)
[Table, PicoGreen Assay]. (2010) (0)
Figure 16, Select examples of cellular IMR90 and percent BSF inhibition data (2011) (0)
Figure 11, Compound interaction with the partially duplex helicase DNA substrate (2013) (0)
Figure 2, Effect of cosolvent on the apparent stability of ML283 (2013) (0)
Figure 3, Stability for compound SID 103147611 (CID 2792221) in 100% aqueous and 50% acetonitrile/aqueous (2013) (0)
Figure 5, Five analogues submitted to support probe SID 88095709 (CID 44640177) (2013) (0)
Figure 2, Graph depicting the stability for ML333/KUC107756 after 48 hours in two separate solvent systems (2013) (0)
SWOT ANALYSIS RESULTS Strategic Initiative #2 Promoting Well-Being, Finding Cures Co-Chairs: (2011) (0)
[Table], EXPERIMENTAL RESULTS FOR SID 123083137 ON OTHER TARGETS (2013) (0)
Figure 12, Rtg3p-GFP translocation assay (2013) (0)
Figure 1, Enzymatic reactions catalyzed by GCase in assays (2013) (0)
Mannich Reactions Using Benzyl Azide as a Latent N-(Phenylamino)methylating Agent. (1998) (0)
Table A7, Critical reagents for the cell viability assay (2013) (0)
Table 5, SAR summary for modification of the R4 substituent (2013) (0)
Figure A2, Carbon data for SID 88095709 (CID 44640177) (2013) (0)
Figure 4, Selected analogs to support probe ML231 (2013) (0)
Table 3, Summary of in vitro ADME properties of ML315 (2013) (0)
[Figure], Primary Screen/Confirmation Triage (2010) (0)
Expression of different adenylyl cyclase isoforms impacts ligand bias downstream of the kappa opioid receptor (2019) (0)
Figure 2, 35S-GTPγS binding assay – Secondary functional assays for KOR agonist probes and selected analogs (2010) (0)
Table 4, Summary of modifications for R2 (2013) (0)
High‐throughput screening for identification of novel allosteric modulators of the D3 dopamine receptor (2015) (0)
Figure 5, TOR compound triage and flow chart (2013) (0)
Selective inhibition of metastasis in vivo, partly through disruption of nucleoli (2019) (0)
Lewis Acid-Mediated Cyclizations of (2′-Amino-N′-tert-butoxycarbonyl-benzylidene)-3-alkenylamines. (1999) (0)
Table 4, Off-target pharmacology data for ML315 highlighting targets with ≥ 50% inhibition or stimulation (2013) (0)
Figure A3, LCMS purity data at 214 nm for SID 99300522 (CID 3392161) (2013) (0)
Table 1, Profile of the Chemical Probe CID2950007 on Ras-Related GTPases (2010) (0)
Table 10, Comparison of solubility and potency for ML283 and selected analogues (2013) (0)
Table 1, Solubility experiments in various media with ML231 and analogs (2013) (0)
Table 11, Summary of in vitro ADME properties of ML283 CID 50930730 (2013) (0)
Figure A6C, High resolution MS for ML336, SID 152199106, CID 71301451 (2013) (0)
Figure 22, CID 50930749 location in cells (2013) (0)
Benzylmorpholine Analogs as Selective Inhibitors of Lung Cytochrome P450 2A13 for the Chemoprevention of Lung Cancer in Tobacco Users (2013) (0)
Cyclizations of Substituted Benzylidene‐3‐alkenylamines: Synthesis of the Tricyclic Core of the Martinellines. (2000) (0)
Figure 11, Stability for compound SID 103904169 (CID 49830258) in 100% aqueous and 50% acetonitrile/aqueous (2013) (0)
Abstract P1-13-08: Inhibition of RNA binding protein HuR function sensitizes the TNBC to chemotherapy (2023) (0)
Figure 11, Triage of HTS hits and progression to meet probe criteria (2011) (0)
Combinatorial Chemistry and Its Associated Technologies (0)
Figure 1, Bioluminescent assays used for Clk4 qHTS (2013) (0)
Table 3, Thiol Stability (DTT) and Plasma Stability for ML370 (2014) (0)
Figure 14, Effects of primuline and P4 (CID 44251437) on NS3 catalyzed peptide cleavage (2013) (0)
AGC Kinase Inhibitors Regulate STING Signaling Through SGK-Dependent and SGK-Independent Mechanisms (2022) (0)
Figure 10, Future SAR studies (2013) (0)
Table 4, Percent of ML336 remaining at the conclusion of the experiment (48h) (2013) (0)
Table 6, Summary of piperazine and combined R4 modifications (X) (2013) (0)
Table 2, Summary of in vitro ADME properties of ML317 (2013) (0)
Abstract 5368: Metarrestin effectively disassembles PNCs and inhibits metastasis (2015) (0)
Figure A6D, LCMS purity data at 214 nM for ML336, SID 152199106, CID 71301451 (2013) (0)
Figure 4, Probe analogs for which samples were submitted to the MLSMR (2013) (0)
Regiochemistry in the Intramolecular Cycloadditions of Substituted 5-Alkenyl and 6-Alkenyl Nitrones. (1986) (0)
Figure 23, Use of fluorescence microscopy to visualize CID 50930730/ML283 in cells (2013) (0)
Inhibitor and Its Use as a Molecular Probe Characterization of a Cdc 42 Protein Cell (2013) (0)
Figure 4, Inhibition of thallium signal in KCNK9-expressing cells by ML308 (2013) (0)
Figure 9, Dose response curves for the active compounds (2013) (0)
Figure 13, HTS scaffolds and associated data prior to validation from resynthesized solid materials (2011) (0)
Table 6, Comparison of Mouse Pharmacokinetics Parameters of Probe after IP Dosing of 50 or 25 mpk in Male C57BL/6 Mice (2010) (0)
Oxazoline and Dihydrooxazine Library (2007) (0)
Hexafluoro‐2‐propanol‐promoted Intramolecular Friedel‐Crafts Acylation (2019) (0)
Abstract 4832: Overcoming breast cancer chemoresistance and blocking metastasis by targeting RNA-binding protein HuR (2016) (0)
Figure 7, Overview of structural variations resulting from SAR efforts (2010) (0)
Figure B3, LCMS purity data at 214 nm for SID 114279600 (CID 50930730); LCMS retention time: 2.68; purity at 214 nm = 93.6% (2013) (0)
Copper‐Catalyzed Oxaziridine‐Mediated Oxidation of C—H Bonds. (2012) (0)
Table 2, SAR summary for compounds with carboxylic acid isosteric replacements (2011) (0)
Figure 16, Validated hit and SAR strategy (2013) (0)
Table 2, Probe and analog submissions to the MLSMR (Evotec) for Identification of Compounds that Reduce PNC Prevalence (2010) (0)
Figure 4, Synthetic route for probe and analogue generation (2013) (0)
Directed regiochemicalcontrolin thering expansion reactionsofasubstituted trans-decalone (1992) (0)
One‐Pot, Regiospecific Assembly of (E)‐Benzamidines from δ‐ and γ‐Amino Acids via an Intramolecular Aminoquinazolinone Rearrangement. (2016) (0)
A Concomitant Allylic Azide Rearrangement/Intramolecular Azide—Alkyne Cycloaddition Sequence. (2014) (0)
Table 8, SAR analysis of P1 derivatives for NS3 helicase inhibitor discovery (2013) (0)
An Enantioselective Synthesis of (-)-Alloyohimban. (1989) (0)
Cytotoxic withanolide constituents of Physalis longifolia (2012) (0)
Table 9, Comparative summary of two current probes CID5236771 & CID44601470 to literature examples (2010) (0)
Table 6, Inhibitory profile of GCase chaperone inhibitors illustrated in Figure 13 (2013) (0)
Abstract 1235: Targeting RNA-binding protein HuR to inhibit human breast cancer invasion and metastasis (2019) (0)
Abstract 867: Blocking breast cancer metastasis by targeting HuR-FOXQ1 signaling axis (2018) (0)
Synthesis and Conformation of Gly—Gly Dipeptides Constrained with Phenylalanine‐Like Aminocaproic Acid Linkers. (2000) (0)
One‐Step Synthesis of Oxazoline and Dihydrooxazine Libraries. (2007) (0)

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