Dale L. Boger
#22,490
Most Influential Person Now
American medicinal and organic chemist
Dale L. Boger's AcademicInfluence.com Rankings
Dale L. Bogerchemistry Degrees
Chemistry
#224
World Rank
#466
Historical Rank
#119
USA Rank
Organic Chemistry
#44
World Rank
#62
Historical Rank
#22
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Chemistry
Dale L. Boger's Degrees
- Bachelors Chemistry University of Kansas
- PhD Chemistry University of Kansas
Why Is Dale L. Boger Influential?
(Suggest an Edit or Addition)According to Wikipedia, Dale Lester Boger is an American medicinal and organic chemist and former chair of the Department of Chemistry at The Scripps Research Institute in La Jolla, CA. Dale Boger was born on August 22, 1953, in Hutchinson, Kansas. He studied chemistry at the University of Kansas , and received his Ph.D. from Harvard University in 1980 under Professor E. J. Corey. Following graduate school, he joined the faculty at the University of Kansas where he became assistant/associate professor of medicinal chemistry .
Dale L. Boger'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
- Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides (1996) (1991)
- Hetero Diels-Alder methodology in organic synthesis (1987) (719)
- Chemical characterization of a family of brain lipids that induce sleep. (1995) (569)
- Diels-Alder reactions of heterocyclic aza dienes. Scope and applications (1986) (513)
- Diels-Alder reactions of azadienes (1983) (489)
- A simple, high-resolution method for establishing DNA binding affinity and sequence selectivity. (2001) (464)
- Reliability of Spike Timing in Neocortical Neurons (1995) (450)
- Reversible Inhibitors of Fatty Acid Amide Hydrolase That Promote Analgesia: Evidence for an Unprecedented Combination of Potency and Selectivity (2004) (332)
- Discovering potent and selective reversible inhibitors of enzymes in complex proteomes (2003) (323)
- Total Syntheses of Ningalin A, Lamellarin O, Lukianol A, and Permethyl Storniamide A Utilizing Heterocyclic Azadiene Diels−Alder Reactions (1999) (317)
- Blockade of Endocannabinoid-Degrading Enzymes Attenuates Neuropathic Pain (2009) (309)
- Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts (2002) (301)
- Disruption of matrix metalloproteinase 2 binding to integrin alpha vbeta 3 by an organic molecule inhibits angiogenesis and tumor growth in vivo. (2001) (268)
- Mechanisms of in situ activation for DNA-targeting antitumor agents. (2002) (256)
- Exceptionally potent inhibitors of fatty acid amide hydrolase: the enzyme responsible for degradation of endogenous oleamide and anandamide. (2000) (249)
- Total synthesis of vinblastine, vincristine, related natural products, and key structural analogues. (2009) (244)
- The Sleep-inducing Lipid Oleamide Deconvolutes Gap Junction Communication and Calcium Wave Transmission in Glial Cells (1997) (236)
- Fe(III)/NaBH4-mediated free radical hydrofluorination of unactivated alkenes. (2012) (223)
- CC-1065 AND THE DUOCARMYCINS : UNDERSTANDING THEIR BIOLOGICAL FUNCTION THROUGH MECHANISTIC STUDIES (1996) (209)
- A fluorescent intercalator displacement assay for establishing DNA binding selectivity and affinity. (2004) (206)
- Iron(III)/NaBH4-mediated additions to unactivated alkenes: synthesis of novel 20'-vinblastine analogues. (2012) (204)
- Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics. (2005) (203)
- Sequence-selective DNA recognition: natural products and nature's lessons. (2004) (192)
- CC-1065 and the Duocarmycins: Synthetic Studies. (1997) (189)
- Total Synthesis of Distamycin A and 2640 Analogues: A Solution-Phase Combinatorial Approach to the Discovery of New, Bioactive DNA Binding Agents and Development of a Rapid, High-Throughput Screen for Determining Relative DNA Binding Affinity or DNA Binding Sequence Selectivity (2000) (165)
- Total synthesis of prodigiosin, prodigiosene, and desmethoxyprodigiosin: Diels-Alder reactions of heterocyclic azadienes and development of an effective palladium(II)-promoted 2,2'-bipyrrole coupling procedure (1988) (165)
- CC-1065 and the duocarmycins: unraveling the keys to a new class of naturally derived DNA alkylating agents. (1995) (165)
- Elucidation of fatty acid amide hydrolase inhibition by potent alpha-ketoheterocycle derivatives from Monte Carlo simulations. (2005) (160)
- Total Synthesis of the Vancomycin Aglycon (1999) (160)
- Direct coupling of catharanthine and vindoline to provide vinblastine: total synthesis of (+)- and ent-(-)-vinblastine. (2008) (156)
- Inverse electron-demand Diels-Alder reactions of N-sulfonyl .alpha.,.beta.-unsaturated imines: a general approach to implementation of the 4.pi. participation of 1-aza-1,3-butadienes in Diels-Alder reactions (1991) (155)
- Acyl radicals: intermolecular and intramolecular alkene addition reactions (1992) (143)
- Solution-phase combinatorial libraries: modulating cellular signaling by targeting protein-protein or protein-DNA interactions. (2003) (137)
- Total synthesis of (-)- and ent-(+)-vindoline and related alkaloids. (2006) (135)
- Partitioning the loss in vancomycin binding affinity for D-Ala-D-Lac into lost H-bond and repulsive lone pair contributions. (2003) (133)
- Total synthesis and evaluation of (.+-.)-N-(tert-butoxycarbonyl)-CBI, (.+-.)-CBI-CDPI1, and (.+-.)-CBI-CDPI2: CC-1065 functional agents incorporating the equivalent 1,2,9,9a-tetrahydrocyclopropa[1,2-c]benz[1,2-e]indol-4-one (CBI) left-hand subunit (1989) (128)
- Asymmetric total synthesis of vindorosine, vindoline, and key vinblastine analogues. (2010) (125)
- Design, synthesis, and evaluation of an alpha-helix mimetic library targeting protein-protein interactions. (2009) (124)
- Oleamide: an endogenous sleep-inducing lipid and prototypical member of a new class of biological signaling molecules. (1998) (124)
- Chemistry and biology of ramoplanin: a lipoglycodepsipeptide with potent antibiotic activity. (2005) (123)
- Peripheral modifications of [Ψ[CH2NH]Tpg4]vancomycin with added synergistic mechanisms of action provide durable and potent antibiotics (2017) (122)
- The mechanism of action of ramoplanin and enduracidin. (2006) (122)
- Chemical requirements for inhibition of gap junction communication by the biologically active lipid oleamide. (1998) (121)
- Fostriecin: chemistry and biology. (2002) (119)
- Total Synthesis of Vinblastine, Related Natural Products, and Key Analogues and Development of Inspired Methodology Suitable for the Systematic Study of Their Structure–Function Properties (2015) (118)
- TLR4/MD-2 activation by a synthetic agonist with no similarity to LPS (2016) (117)
- An in vitro and in vivo disconnect uncovered through high-throughput identification of botulinum neurotoxin A antagonists (2007) (115)
- Asymmetric total synthesis of vindoline. (2010) (115)
- Total synthesis of ningalin B utilizing a heterocyclic azadiene Diels-Alder reaction and discovery of a new class of potent multidrug resistant (MDR) reversal agents. (2000) (115)
- Asymmetric total synthesis of ent-(-)-roseophilin: assignment of absolute configuration. (2001) (114)
- A general solution to implementing the 4.pi. participation of 1-aza-1,3-butadienes in Diels-Alder reactions: inverse electron demand Diels-Alder reactions of .alpha..beta.-unsaturated N-benzenesulfonyl imines (1989) (113)
- An Efficient Synthesis of 1,2,9,9a-Tetrahydrocyclopropa[c]benz[e]indol-4-one CBI: An Enhanced and Simplified Analog of the CC-1065 and Duocarmycin Alkylation Subunits (1995) (112)
- The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH). (2011) (112)
- A redesigned vancomycin engineered for dual D-Ala-D-ala And D-Ala-D-Lac binding exhibits potent antimicrobial activity against vancomycin-resistant bacteria. (2011) (111)
- Fatty acid amide signaling molecules. (2010) (111)
- Total synthesis and evaluation of [Psi[CH2NH]Tpg4]vancomycin aglycon: reengineering vancomycin for dual D-Ala-D-Ala and D-Ala-D-Lac binding. (2006) (109)
- Inverse electron demand Diels-Alder reactions of heterocyclic azadienes: formal total synthesis of streptonigrin (1985) (108)
- Streptonigrin and lavendamycin partial structures. Probes for the minimum, potent pharmacophore of streptonigrin, lavendamycin, and synthetic quinoline-5,8-diones. (1987) (108)
- Shape-Dependent Catalysis: Insights into the Source of Catalysis for the CC-1065 and Duocarmycin DNA Alkylation Reaction (1999) (108)
- Inhibition of Oleamide Hydrolase Catalyzed Hydrolysis of the Endogenous Sleep-Inducing Lipid cis-9-Octadecenamide (1996) (107)
- Novel Solution Phase Strategy for the Synthesis of Chemical Libraries Containing Small Organic Molecules (1996) (107)
- Azadiene diels‐alder reactions: Scope and applications. Total synthesis of natural and Ent‐fredericamycin A (1995) (105)
- Trifluoromethyl ketone inhibitors of fatty acid amide hydrolase: a probe of structural and conformational features contributing to inhibition. (1999) (103)
- Duocarmycin-pyrindamycin DNA alkylation properties and identification, synthesis, and evaluation of agents incorporating the pharmacophore of the duocarmycin-pyrindamycin alkylation subunit. Identification of the CC-1065 duocarmycin common pharmacophore (1990) (102)
- Vancomycin, teicoplanin, and ramoplanin: Synthetic and mechanistic studies † (2001) (102)
- Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition. (2003) (102)
- Bleomycin: Synthetic and Mechanistic Studies. (1999) (102)
- Total Syntheses of Vancomycin-Related Glycopeptide Antibiotics and Key Analogues. (2017) (101)
- Diastereoselective Total Synthesis of the Vancomycin Aglycon with Ordered Atropisomer Equilibrations (1999) (101)
- Fundamental relationships between structure, reactivity, and biological activity for the duocarmycins and CC-1065. (2009) (99)
- Fatty acid amide hydrolase substrate specificity. (2000) (98)
- First and second generation total synthesis of the teicoplanin aglycon. (2001) (98)
- Intramolecular Diels-Alder and tandem intramolecular Diels-Alder/1,3-dipolar cycloaddition reactions of 1,3,4-oxadiazoles. (2002) (97)
- Unique Small Molecule Entry Inhibitors of Hemorrhagic Fever Arenaviruses* (2008) (96)
- Inverse electron demand Diels-Alder reactions of 1,2,3-triazines: pronounced substituent effects on reactivity and cycloaddition scope. (2011) (96)
- The fatty acid amide hydrolase (FAAH) inhibitor PF‐3845 acts in the nervous system to reverse LPS‐induced tactile allodynia in mice (2012) (95)
- Total synthesis of [Ψ[C(═S)NH]Tpg4]vancomycin aglycon, [Ψ[C(═NH)NH]Tpg4]vancomycin aglycon, and related key compounds: reengineering vancomycin for dual D-Ala-D-Ala and D-Ala-D-Lac binding. (2012) (95)
- Total synthesis of (±)-N2-(phenylsulfonyl)-CPI, (±)-CC-1065, (+)-CC-1065, ent-(−)-CC-1065, and the precise, functional agents (±)-CPI-CDPI2, (+)-CPI-CDPI2, and (−)-CPI-CDPI2 [(±)-(3bR*, 4aS*)-, (+)-(3bR,4aS)-, and (−)-(3bS,4aR)-deoxy-CC-1065] (1988) (93)
- Redesign of glycopeptide antibiotics: back to the future. (2012) (93)
- Intramolecular diels-alder/1,3-dipolar cycloaddition cascade of 1,3,4-oxadiazoles. (2006) (93)
- Total Synthesis of Bouvardin, O-Methylbouvardin, and O-Methyl-N9-desmethylbouvardin (1994) (91)
- Structural requirements for 5-HT2A and 5-HT1A serotonin receptor potentiation by the biologically active lipid oleamide. (1998) (90)
- Total synthesis of (-)- and ent-(+)-vindoline. (2005) (90)
- Cerebrodiene: a brain lipid isolated from sleep-deprived cats. (1994) (90)
- Synthesis of N-(tert-butyloxycarbonyl)-CBI, CBI, CBI-CDPI1, and CBI-CDPI2: enhanced functional analogs of CC-1065 incorporating the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) left-hand subunit (1990) (90)
- Behavioral evidence for the interaction of oleamide with multiple neurotransmitter systems. (2001) (89)
- Comprehensive peptidomimetic libraries targeting protein-protein interactions. (2012) (89)
- Total synthesis of (+)-fendleridine (aspidoalbidine) and (+)-1-acetylaspidoalbidine. (2010) (89)
- Thermal reactions of cyclopropenone ketals: key mechanistic features and scope of the cycloaddition reactions of delocalized singlet vinylcarbenes: three-carbon 1,1-/1,3-dipoles (1986) (88)
- Intramolecular Diels-Alder reactions of 1,2-diazines: general indoline synthesis. Studies on the preparation of the central and right-hand segments of CC-1065 (1984) (88)
- Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity. (2005) (88)
- Inverse electron demand Diels-Alder reactions of heterocyclic azadienes. Studies on the total synthesis of lavendamycin: investigative studies on the preparation of the CDE .beta.-carboline ring system and AB quinoline-5,8-quinone ring system (1985) (87)
- Structure Determination of an Endogenous Sleep-Inducing Lipid, cis-9-Octadecenamide (Oleamide): A Synthetic Approach to the Chemical Analysis of Trace Quantities of a Natural Product (1996) (86)
- Total synthesis of fostriecin (CI-920). (2001) (85)
- Generalized Dipeptidomimetic Template: Solution Phase Parallel Synthesis of Combinatorial Libraries (1996) (85)
- Inverse electron demand Diels-Alder reactions of 3,6-bis(methylthio)-1,2,4,5-tetrazine. 1,2-Diazine introduction and direct implementation of a divergent 1,2,4,5-tetrazine .fwdarw. 1,2-diazine .fwdarw. benzene (indoline/indole) Diels-Alder strategy (1988) (84)
- A Pd(0)-mediated indole (macro)cyclization reaction. (2013) (84)
- Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase. (2008) (84)
- Total Synthesis of Bleomycin A2 and Related Agents. 4. Synthesis of the Disaccharide Subunit 2-O-(3-O-Carbamoyl-.alpha.-D-mannopyranosyl)-L-gulopyranose and Completion of the Total Synthesis of Bleomycin A2 (1994) (84)
- Diels-Alder reactions of heterocyclic azadienes: total synthesis of PDE I, PDE II, and PDE I dimer methyl ester (1987) (83)
- (+)- and ent-(-)-Duocarmycin SA and (+)- and ent-(-)-N-BOC-DSA DNA Alkylation Properties.Alkylation Site Models That Accommodate the Offset AT-Rich Adenine N3 Alkylation Selectivity of the Enantiomeric Agents (1994) (83)
- Total synthesis of the ramoplanin A2 and ramoplanose aglycon. (2002) (82)
- Total synthesis of azafluoranthene alkaloids: rufescine and imeluteine (1984) (82)
- Binding and inactivation mechanism of a humanized fatty acid amide hydrolase by alpha-ketoheterocycle inhibitors revealed from cocrystal structures. (2009) (82)
- Endocannabinoid Modulation of Scratching Response in an Acute Allergenic Model: A New Prospective Neural Therapeutic Target for Pruritus (2009) (81)
- Thiazole orange as the fluorescent intercalator in a high resolution fid assay for determining DNA binding affinity and sequence selectivity of small molecules. (2001) (81)
- Total Synthesis of Phomazarin (1999) (80)
- Total synthesis of ningalin D. (2005) (80)
- Total synthesis of chloropeptin II (complestatin) and chloropeptin I. (2009) (78)
- The Duocarmycins: Synthetic and Mechanistic Studies (1995) (75)
- Diastereoselective Diels-Alder reactions of N-sulfonyl-1-aza-1,3-butadienes with optically active enol ethers: an asymmetric variant of the 1-azadiene Diels-Alder reaction. (2006) (75)
- Diels-Alder reaction of heterocyclic azadienes. I. Thermal cycloaddition of 1,2,4-triazine with enamines: simple preparation of substituted pyridines (1981) (75)
- Total synthesis of lavendamycin methyl ester (1985) (74)
- SYNTHESIS OF THE VANCOMYCIN CD AND DE RING SYSTEMS (1997) (73)
- (-)-SANDRAMYCIN : TOTAL SYNTHESIS AND CHARACTERIZATION OF DNA BINDING PROPERTIES (1996) (72)
- Total syntheses of thiocoraline and BE-22179 and assessment of their DNA binding and biological properties. (2001) (71)
- Total synthesis of (-)- and ent-(+)-vindorosine: tandem intramolecular Diels-Alder/1,3-dipolar cycloaddition of 1,3,4-oxadiazoles. (2006) (71)
- An alternative and convenient strategy for generation of substantial quantities of singly 5'-32P-end-labeled double-stranded DNA for binding studies: development of a protocol for examination of functional features of (+)-CC-1065 and the duocarmycins that contribute to their sequence-selective DNA a (1991) (71)
- Room-temperature, endo-specific 1-aza-1,3-butadiene Diels-Alder reactions: acceleration of the LUMOdiene-controlled [4 + 2] cycloaddition reactions through noncomplementary aza diene substitution (1990) (70)
- Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti–PD-L1 to eliminate melanoma in mice (2018) (70)
- Synthesis and preliminary evaluation of agents incorporating the pharmacophore of the duocarmycin/pyrindamycin alkylation subunit: identification of the CC-1065/duocarmycin common pharmacophore (1990) (70)
- Thermal cycloaddition of dimethyl 1,2,4,5-tetrazine-3,6-dicarboxylate with electron-rich olefins: 1,2-diazine and pyrrole introduction ― Preparation of octamethylporphin (OMP) (1984) (70)
- Total Synthesis of Natural (−)- and ent-(+)-4-Desacetoxy-6,7-dihydrovindorosine and Natural and ent-Minovine: Oxadiazole Tandem Intramolecular Diels−Alder/1,3-Dipolar Cycloaddition Reaction (2005) (70)
- Total synthesis, structure revision, and absolute configuration of (+)-yatakemycin. (2004) (69)
- α-Keto heterocycle inhibitors of fatty acid amide hydrolase: carbonyl group modification and α-substitution (2001) (69)
- A detailed, convenient preparation of dimethyl 1,2,4,5-tetrazine-3,6-dicarboxylate (1985) (68)
- A convenient and general preparation of N-sulfonylimines (1992) (67)
- Total synthesis of the ristocetin aglycon. (2004) (67)
- Potent and Selective α-Ketoheterocycle-Based Inhibitors of the Anandamide and Oleamide Catabolizing Enzyme, Fatty Acid Amide Hydrolase (2007) (67)
- Two novel 1,2,4,5-tetrazines that participate in inverse electron demand Diels-Alder reactions with an unexpected regioselectivity. (2006) (66)
- Tandem Intramolecular Diels-Alder/1,3-Dipolar Cycloaddition Cascade of 1,3,4-Oxadiazoles: Initial Scope and Applications. (2016) (65)
- Synthesis and evaluation of aborted and extended CC-1065 functional analogs: (+)- and (-)-CPI-PDE-I1, (+)- and (-)-CPI-CDPI1, and (.+-.)-, (+)-, and (-)-CPI-CDPI3. Preparation of key partial structures and definition of an additional functional role of the CC-1065 central and right-hand subunits (1990) (65)
- Regioselective Inverse Electron Demand Diels-Alder Reactions of N-Acyl 6-Amino-3-(methylthio)-1,2,4,5-tetrazines. (1998) (65)
- Diels-Alder reaction of heterocyclic azadienes. 2. "Catalytic" Diels-Alder reaction of in situ generated enamines with 1,2,4-triazines: general pyridine annulation (1982) (65)
- Diels-Alder reactions of N-sulfonyl-1-aza-1,3-butadienes : development of a synthetic approach to the streptonigrone C ring (1991) (64)
- Total synthesis of piericidin A1 and B1. (2005) (64)
- Total Synthesis of Bleomycin A2 and Related Agents. 1. Synthesis and DNA Binding Properties of the Extended C-Terminus: Tripeptide S, Tetrapeptide S, Pentapeptide S, and Related Agents (1994) (64)
- Catalysis of the CC-1065 and duocarmycin DNA alkylation reaction: DNA binding induced conformational change in the agent results in activation. (1997) (64)
- Total synthesis of (+)-CC-1065 and ent-(-)-CC-1065 (1988) (63)
- Diels-Alder reactions of 1-aza-1,3-butadienes: room temperature, endo-selective LUMOdiene-controlled [4 + 2] cycloaddition reactions of N-sulfonyl-4-(ethoxycarbonyl)-1-aza-1,3-butadienes (1990) (63)
- Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions. (2011) (63)
- Asymmetric total synthesis of (+)- and ent-(-)-yatakemycin and duocarmycin SA: evaluation of yatakemycin key partial structures and its unnatural enantiomer. (2006) (62)
- Total Syntheses of (−)-Kopsifoline D and (−)-Deoxoapodine: Divergent Total Synthesis via Late-Stage Key Strategic Bond Formation (2014) (62)
- Erythropoietin mimetics derived from solution phase combinatorial libraries. (2002) (62)
- Total synthesis of complestatin: development of a Pd(0)-mediated indole annulation for macrocyclization. (2010) (62)
- Total Synthesis of [Ψ[C(=NH)NH]Tpg4]Vancomycin and its (4-Chlorobiphenyl)methyl Derivative: Impact of Peripheral Modifications on Vancomycin Analogues Redesigned for Dual d-Ala-d-Ala and d-Ala-d-Lac Binding (2014) (61)
- Isolation and characterization of the duocarmycin-adenine DNA adduct (1991) (61)
- Total synthesis of (+)-duocarmycin SA (1992) (61)
- Structure−Activity Relationships of α-Ketooxazole Inhibitors of Fatty Acid Amide Hydrolase (2007) (61)
- N-acylglycine amidation: implications for the biosynthesis of fatty acid primary amides. (1999) (61)
- Total synthesis of cycloisodityrosine, RA-VII, deoxybouvardin, and N29-desmethyl-RA-VII: Identification of the pharmacophore and reversal of the subunit functional roles (1993) (61)
- DNA alkylation properties of yatakemycin. (2003) (61)
- A convenient preparation of 2-substituted benzothiazoles (1978) (61)
- Total synthesis and evaluation of a key series of C5-substituted vinblastine derivatives. (2010) (61)
- Total Synthesis of the Teicoplanin Aglycon (2000) (60)
- Total synthesis of (.+-.)-cis and (.+-.)-trans-Trikentrin A: Diels-Alder reactions of heteroaromatic azadienes (1991) (59)
- Vancomycin and ristocetin models: synthesis via the Ullmann macrocyclization reaction (1993) (59)
- Identification of a novel class of small-molecule antiangiogenic agents through the screening of combinatorial libraries which function by inhibiting the binding and localization of proteinase MMP2 to integrin alpha(V)beta(3). (2001) (58)
- Inverse electron demand Diels-Alder reactions of 3-carbomethoxy-2-pyrones. Controlled introduction of oxygenated aromatics: benzene, phenol, catechol, resorcinol, and pyrogallol annulation. Regiospecific total synthesis of sendaverine and a preparation of 6,7-benzomorphans (1984) (58)
- Scope of the inverse electron demand Diels-Alder reactions of 1,2,3-triazine. (2011) (58)
- Accelerated inverse electron demand Diels-Alder reactions of 1-oxa-1,3-butadienes: [4 + 2] cycloaddition reactions of .beta.,.gamma.-unsaturated .alpha.-keto esters (1988) (57)
- Synthesis and Evaluation of CC-1065 and Duocarmycin Analogues Incorporating the Iso-CI and Iso-CBI Alkylation Subunits: Impact of Relocation of the C-4 Carbonyl (1997) (57)
- CBI-TMI: Synthesis and Evaluation of a Key Analog of the Duocarmycins. Validation of a Direct Relationship between Chemical Solvolytic Stability and Cytotoxic Potency and Confirmation of the Structural Features Responsible for the Distinguishing Behavior of Enantiomeric Pairs of Agents (1994) (57)
- Total synthesis of piericidin A1 and B1 and key analogues. (2006) (56)
- Total synthesis of kopsinine. (2013) (56)
- Acyl radicals: functionalized free radicals for intramolecular cyclization reactions (1988) (55)
- An endogenous sleep-inducing compound is a novel competitive inhibitor of fatty acid amide hydrolase. (1998) (55)
- Total synthesis of anhydrolycorinone utilizing sequential intramolecular Diels-Alder reactions of a 1,3,4-oxadiazole. (2002) (55)
- A remarkable series of vinblastine analogues displaying enhanced activity and an unprecedented tubulin binding steric tolerance: C20' urea derivatives. (2013) (55)
- Total synthesis of lycogarubin C and lycogalic acid. (2010) (55)
- Molecular basis for sequence selective DNA alkylation by (+)- and ent-(-)-CC-1065 and related agents: alkylation site models that accommodate the offset AT-rich adenine N3 alkylation selectivity. (1994) (55)
- Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. (2008) (54)
- Tandem free-radical alkene addition reactions of acyl radicals (1990) (54)
- Total synthesis of Amaryllidaceae alkaloids utilizing sequential intramolecular heterocyclic azadiene Diels-Alder reactions of an unsymmetrical 1,2,4,5-tetrazine. (2000) (53)
- A unique class of duocarmycin and CC-1065 analogues subject to reductive activation. (2007) (53)
- A solution-phase strategy for the synthesis of chemical libraries containing small organic molecules: a universal and dipeptide mimetic template. (1996) (53)
- Reversed and Sandwiched Analogs of Duocarmycin SA: Establishment of the Origin of the Sequence-Selective Alkylation of DNA and New Insights into the Source of Catalysis (1997) (53)
- Synthesis and inverse electron demand Diels-Alder reactions of 3,6-bis(3,4-dimethoxybenzoyl)-1,2,4,5-tetrazine. (2003) (53)
- Alkylation of duplex DNA in nucleosome core particles by duocarmycin SA and yatakemycin (2006) (53)
- Phenyl selenoesters as effective precursors of acyl radicals for use in intermolecular alkene addition reactions (1989) (53)
- Total synthesis of L,L-isodityrosine and isodityrosine-derived agents: K-13, OF4949-III, and OF4949-IV (1990) (52)
- Intramolecular acyl radical-alkene addition reactions: macrocyclization reactions (1990) (52)
- Total syntheses and initial evaluation of [Ψ[C(═S)NH]Tpg⁴]vancomycin, [Ψ[C(═NH)NH]Tpg⁴]vancomycin, [Ψ[CH₂NH]Tpg⁴]vancomycin, and their (4-chlorobiphenyl)methyl derivatives: synergistic binding pocket and peripheral modifications for the glycopeptide antibiotics. (2015) (52)
- Two comparisons of the performance of positional scanning and deletion synthesis for the identification of active constituents in mixture combinatorial libraries. (2000) (52)
- Total synthesis of chlorofusin, its seven chromophore diastereomers, and key partial structures. (2008) (51)
- d,l- and meso-Isochrysohermidin: total synthesis and interstrand DNA crosslinking (1993) (51)
- Synthesis of N-(phenylsulfonyl)-CI, N-((tert-butyloxy)carbonyl)-CI, CI-CDPI1, and CI-CDPI2: CC-1065 functional analog incorporating the parent 1,2,7,71-tetrahydrocycloprop[1,2-c]indol-4-one (CI) left-hand subunit (1990) (51)
- Thermal reactions of cyclopropenone ketals: application of the cycloaddition reactions of delocalized singlet vinylcarbenes: three-carbon 1,1-/1,3-dipoles: an alternative synthesis of deacetamidocolchiceine: formal total synthesis of colchicine (1986) (51)
- Oxidative cationic cyclization reactions effected by pyridinium chlorochromate (1978) (51)
- Total synthesis and evaluation of vinblastine analogues containing systematic deep-seated modifications in the vindoline subunit ring system: core redesign. (2013) (51)
- Total Synthesis of Nothapodytine B and (−)-Mappicine (1998) (51)
- Delineation of a fundamental alpha-ketoheterocycle substituent effect for use in the design of enzyme inhibitors. (2006) (51)
- Divergent total syntheses of (-)-aspidospermine and (+)-spegazzinine. (2012) (51)
- Thermal cycloaddition of 1,3,5-triazine with enamines: regiospecific pyrimidine annulation (1982) (51)
- 4.3 – Heterodiene Additions (1991) (50)
- Yatakemycin: total synthesis, DNA alkylation, and biological properties. (2008) (50)
- Design and synthesis of a conformational analog of deoxybouvardin (1991) (50)
- Total synthesis of deoxybouvardin and RA-VII: macrocyclization via an intramolecular Ullmann reaction (1991) (49)
- Small molecule inhibitors of Myc/Max dimerization and Myc-induced cell transformation. (2009) (49)
- X-ray crystallographic analysis of alpha-ketoheterocycle inhibitors bound to a humanized variant of fatty acid amide hydrolase. (2010) (49)
- Enantioselective Total Synthesis of (+)-Duocarmycin A, epi-(+)-Duocarmycin A, and Their Unnatural Enantiomers (1996) (49)
- Total Synthesis of the Rubrolone Aglycon (2000) (49)
- An improved synthesis of 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI): a simplified analog of the CC-1065 alkylation subunit (1992) (49)
- 10'-Fluorovinblastine and 10'-Fluorovincristine: Synthesis of a Key Series of Modified Vinca Alkaloids. (2011) (49)
- A demonstration of the intrinsic importance of stabilizing hydrophobic binding and non-covalent van der Waals contacts dominant in the non-covalent CC-1065/B-DNA binding. (1990) (49)
- ROLE OF THE CC-1065 AND DUOCARMYCIN N2 SUBSTITUENT : VALIDATION OF A DIRECT RELATIONSHIP BETWEEN SOLVOLYSIS CHEMICAL STABILITY AND IN VITRO BIOLOGICAL POTENCY (1994) (49)
- Inverse Electron Demand Diels-Alder Reactions of Heterocyclic Azadienes, 1-Aza-1,3-Butadienes, Cyclopropenone Ketals, and Related Systems. A Retrospective. (2019) (49)
- Total Synthesis of Streptonigrone. (1993) (49)
- Structure-Activity Relationship Studies of Fostriecin, Cytostatin, and Key Analogs, with PP1, PP2A, PP5, and (β12–β13)-Chimeras (PP1/PP2A and PP5/PP2A), Provide Further Insight into the Inhibitory Actions of Fostriecin Family Inhibitors (2009) (49)
- Total synthesis and preliminary evaluation of (+)- and ent-(−)-duocarmycin SA (1993) (49)
- Duocarmycin SA Shortened, Simplified, and Extended Agents: A Systematic Examination of the Role of the DNA Binding Subunit (1997) (47)
- Total Synthesis of Bleomycin A2 and Related Agents. 2. Synthesis of (-)-Pyrimidoblamic Acid, epi-(+)-Pyrimidoblamic Acid, (+)-Desacetamidopyrimidoblamic Acid, and (-)-Descarboxamidopyrimidoblamic Acid (1994) (47)
- CDPI3-enediyne and CDPI3-EDTA conjugates: a new class of DNA cleaving agents (1993) (46)
- Tandem free-radical ring expansion and 5-exo-dig 5-hexynyl radical cyclization: a useful approach to fused bicyclic carbocycles (1990) (46)
- Silver(I)-promoted conversion of thioamides to amidines: divergent synthesis of a key series of vancomycin aglycon residue 4 amidines that clarify binding behavior to model ligands. (2012) (46)
- New insights into the mechanism and an expanded scope of the Fe(III)-mediated vinblastine coupling reaction. (2012) (46)
- Determination of the Relative and Absolute Stereochemistry of Fostriecin (CI-920) (1997) (45)
- Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics. (2011) (45)
- Reversibility of the duocarmycin A and SA DNA alkylation reaction (1993) (45)
- Total Synthesis of (+)-Duocarmycin A, epi-(+)-Duocarmycin A and Their Unnatural Enantiomers: Assessment of Chemical and Biological Properties (1997) (45)
- DNA alkylation properties of enhanced functional analogs of CC-1065 incorporating the 1,2,9,9a-tetrahydrocyclopropa[1,2-c]benz[1,2-e]indol-4-one (CBI) alkylation subunit (1992) (44)
- An effective, thermal three-carbon + two-carbon cycloaddition for cyclopentenone formation: formal 1,3-dipolar cycloaddition of cyclopropenone ketals (1984) (44)
- Potent Vinblastine C20' Ureas Displaying Additionally Improved Activity Against a Vinblastine-Resistant Cancer Cell Line. (2013) (44)
- Total synthesis of prodigiosin (1987) (44)
- Inverse Electron Demand Diels-Alder Reactions of 2,4,6-(ethoxycarbonyl)-l,3,5-triazine and 2,4,6-(methylthio)-1,3,5-triazine: Pyrimidine Introduction (1988) (43)
- 1,2,9,9a-Tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) analogs of CC-1065 and the duocarmycins: synthesis and evaluation. (1995) (42)
- Alanine scan of [L-Dap(2)]ramoplanin A2 aglycon: assessment of the importance of each residue. (2007) (42)
- Total synthesis of K-13 (1989) (42)
- Total synthesis and evaluation of cytostatin, its C10-C11 diastereomers, and additional key analogues: impact on PP2A inhibition. (2006) (42)
- Total syntheses of (+)-P-3A, epi-(-)-P-3A, and (-)-desacetamido P-3A (1994) (42)
- Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid. (2003) (42)
- A Specific Interaction of Small Molecule Entry Inhibitors with the Envelope Glycoprotein Complex of the Junín Hemorrhagic Fever Arenavirus* (2010) (42)
- Resolution of a CBI precursor and incorporation into the synthesis of (+)-cbi, (+)-CBI-CDPI1, (+)-CBI-CDPI2: enhanced functional analogs of (+)-CC-1065. A critical appraisal of a proposed relationship between electrophile reactivity, DNA binding properties, and cytotoxic potency. (1990) (42)
- Catalysis of Heterocyclic Azadiene Cycloaddition Reactions by Solvent Hydrogen Bonding: Concise Total Synthesis of Methoxatin. (2016) (41)
- Catharanthine C16 substituent effects on the biomimetic coupling with vindoline: preparation and evaluation of a key series of vinblastine analogues. (2010) (41)
- (+)-CC 1065 DNA alkylation : key studies demonstrating a noncovalent binding selectivity contribution to the alkylation selectivity (1991) (41)
- Total synthesis and examination of three key analogues of ramoplanin: a lipoglycodepsipeptide with potent antibiotic activity. (2004) (41)
- Functional analogs of CC-1065 and the duocarmycins incorporating the 9a-(chloromethyl)-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (C2BI) alkylation subunit: synthesis and preliminary DNA alkylation studies (1992) (40)
- Structural Basis of TLR2/TLR1 Activation by the Synthetic Agonist Diprovocim. (2019) (40)
- Synthesis, chemical properties, and biological evaluation of CC-1065 and duocarmycin analogues incorporating the 5-methoxycarbonyl-1,2,9,9a-tetrahydrocyclopropa. (2001) (40)
- Studies on the total synthesis of CC-1065: preparation of a synthetic simplified 3-carbamoyl-1,2-dihydro-3H-pyrrolo[3,2-e]indole dimer/trimer/tetramer (CDPI dimer/trimer/tetramer) and development of methodology for PDE-I dimer methyl ester formation (1987) (40)
- Synthesis of (R)-(4-Methoxy-3,5-dihydroxyphenyl)glycine Derivatives: The Central Amino Acid of Vancomycin and Related Agents (1996) (40)
- Synthesis, Chemical Properties, and Preliminary Evaluation of Substituted CBI Analogs of CC-1065 and the Duocarmycins Incorporating the 7-Cyano-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one Alkylation Subunit: Hammett Quantitation of the Magnitude of Electronic Effects on Functional Reactivity (1996) (39)
- Studies on the total synthesis of bouvardin and deoxybouvardin: cyclic hexapeptide cyclization studies and preparation of key partial structures (1988) (39)
- Divergent de novo synthesis of carbohydrates based on an accelerated inverse electron demand Diels-Alder reaction of 1-oxa-1,3-butadienes (1988) (39)
- Diels-Alder reactions of heterocyclic azadienes: total synthesis of PDE-II methyl ester (1986) (39)
- Total synthesis of (+)-Piperazinomycin (1993) (39)
- Multidrug resistance reversal activity of permethyl ningalin B amide derivatives. (2004) (39)
- Total Synthesis of (-)-Vindoline and (+)-4-epi-Vindoline Based on a 1,3,4-Oxadiazole Tandem Intramolecular [4 + 2]/[3 + 2] Cycloaddition Cascade Initiated by an Allene Dienophile. (2015) (39)
- Total synthesis and biological properties of novel antineoplastic (chloromethyl)furanoindolines: an asymmetric hydroboration mediated synthesis of the alkylation subunits. (1994) (39)
- Demonstration of a pronounced effect of noncovalent binding selectivity on the (+)-CC-1065 DNA alkylation and identification of the pharmacophore of the alkylation subunit. (1991) (39)
- Cycloadditions of Noncomplementary Substituted 1,2,3-Triazines (2014) (39)
- Solution-phase parallel synthesis of a pharmacophore library of HUN-7293 analogues: a general chemical mutagenesis approach to defining structure-function properties of naturally occurring cyclic (depsi)peptides. (2002) (38)
- Total synthesis of combretastatin D-2: intramolecular Ullmann macrocyclization reaction (1991) (38)
- Synthesis and Properties of Substituted CBI Analogs of CC-1065 and the Duocarmycins Incorporating the 7-Methoxy-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (MCBI) Alkylation Subunit: Magnitude of Electronic Effects on the Functional Reactivity. (1996) (38)
- Regioselectivity of the intermolecular Diels-Alder reaction of acyl nitroso compounds (C-nitrosocarbonyl compounds) and nitrosoformates (O-nitrosocarbonyl compounds). Preparation of functionalized cis-.DELTA.6-1-octalones (1985) (38)
- Synthesis, X-ray Structure, and Properties of Fluorocyclopropane Analogs of the Duocarmycins Incorporating the 9,9-Difluoro-1,2,9,9a-tetrahydrocyclopropa[c]benzo[e]indol-4-one (F2CBI) Alkylation Subunit (1996) (38)
- Systematic exploration of the structural features of yatakemycin impacting DNA alkylation and biological activity. (2007) (37)
- Studies of the total synthesis of fredericamycin A. Preparation of key partial structures and development of an intermolecular alkyne-chromium carbene complex benzannulation cyclization approach to the ABCD(E) ring system (1990) (37)
- Inverse Electron Demand Diels-Alder Reactions of Heterocyclic Azadienes: [4 + 2] Cycloaddition Reaction of Amidines with 1,3,5-Triazines (1994) (37)
- Thermal Atropisomerism of Aglucovancomycin Derivatives: Preparation of (M,M,M)- and (P,M,M)-Aglucovancomycins (1998) (37)
- Total synthesis and comparative evaluation of luzopeptin A-C and quinoxapeptin A-C (1999) (37)
- Regiospecific total synthesis of juncusol (1984) (37)
- DNA alkylation properties of the duocarmycins: (+)-duocarmycin A, epi-(+)-duocarmycin A, ent-(−)-duocarmycin A and epi,ent-(−)-duocarmycin A (1992) (36)
- The isolation, total synthesis and structure elucidation of chlorofusin, a natural product inhibitor of the p53-mDM2 protein-protein interaction. (2009) (36)
- Intramolecular ullmann condensation reaction : an effective approach to macrocyclic Diaryl Ethers (1991) (36)
- Asymmetric Synthesis of Orthogonally Protected l-threo-β-Hydroxyasparagine (2000) (36)
- Total Syntheses of (−)-Pyrimidoblamic Acid and P-3A (2014) (36)
- Total synthesis and evaluation of iso-duocarmycin SA and iso-yatakemycin. (2009) (36)
- (+)-CC-1065 DNA alkylation : observation of an unexpected relationship between cyclopropane electrophile reactivity and the intensity of DNA alkylation (1991) (36)
- Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase. (2008) (36)
- Formal total synthesis of streptonigrin (1983) (36)
- Synthesis of the lower subunit of rhizoxin (1992) (35)
- Synthesis of (9R,12S)- and (9S,12S)-Cycloisodityrosine and Their N-Methyl Derivatives. (1997) (35)
- Transannular Diels-Alder/1,3-dipolar cycloaddition cascade of 1,3,4-oxadiazoles: total synthesis of a unique set of vinblastine analogues. (2013) (35)
- High resolution solution structure of a DNA duplex alkylated by the antitumor agent duocarmycin SA. (1997) (35)
- Synthesis and preliminary evaluation of the fredericamycin A ABCDE ring system (1991) (35)
- Induction of endonucleolytic DNA fragmentation and apoptosis by the duocarmycins (1994) (35)
- Benzothiazoles as carbonyl equivalents (1978) (35)
- Diels-alder cycloaddition reactions of cyclopropenone ketals : Dual participation in inverse electron demand (lumodiene controlled) and normal (homodiene controlled) diels-alder reactions. Approaches to the preparation of tropones (1986) (35)
- Total Synthesis of Luzopeptins A−C (1999) (35)
- Synthesis of CC-1065 and duocarmycin analogs via intramolecular aryl radical cyclization of a tethered vinyl chloride (1998) (35)
- Total Synthesis of Bleomycin A2 and Related Agents. 3. Synthesis and Comparative Evaluation of Deglycobleomycin A2,Epideglycobleomycin A2, Deglycobleomycin A1, and Desacetamido-, Descarboxamido-, Desmethyl-, and Desimidazolyldeglycobleomycin A2 (1994) (34)
- Singlet oxygen oxidation of bipyrroles: total synthesis of d,l- and meso-isochrysohermidin (1993) (34)
- New insights into inhibitor design from the crystal structure and NMR studies of Escherichia coli GAR transformylase in complex with beta-GAR and 10-formyl-5,8,10-trideazafolic acid. (1999) (34)
- 4.pi. Participation of 1-aza-1,3-butadienes in [4 + 2] cycloaddition reactions: intramolecular Diels-Alder reactions of .alpha.,.beta.-unsaturated N-sulfonylimines (1993) (34)
- Synthesis and chiroptical properties of some asymmetric planar cisoid dienes (1976) (34)
- Preparation and inverse electron demand Diels-Alder reactions of 3-methoxy-6-methylthio-1,2,4,5-tetrazine (1997) (34)
- A Fluorescent Intercalator Displacement Assay for Establishing DNA Binding Selectivity and Affinity (2005) (33)
- Synthesis of a Potent Vinblastine: Rationally Designed Added Benign Complexity. (2016) (33)
- Multidrug resistance reversal activity of key ningalin analogues. (2003) (33)
- Potent reversal of multidrug resistance by ningalins and its use in drug combinations against human colon carcinoma xenograft in nude mice (2005) (33)
- SYNTHESIS AND EVALUATION OF A CARBOCYCLIC ANALOGUE OF THE CC-1065 AND DUOCARMYCIN ALKYLATION SUBUNITS : ROLE OF THE VINYLOGOUS AMIDE AND IMPLICATIONS ON DNA ALKYLATION CATALYSIS (1998) (33)
- Total synthesis and structure of the ramoplanin A1 and A3 aglycons: two minor components of the ramoplanin complex. (2004) (33)
- Synthesis and Evaluation of CC-1065 and Duocarmycin Analogs Incorporating the 1,2,3,4,11,11a-Hexahydrocyclopropa[c]naphtho[2,1-b]azepin-6-one (CNA) Alkylation Subunit: Structural Features that Govern Reactivity and Reaction Regioselectivity (1997) (32)
- Fluoride-mediated capture of a noncovalent bound state of a reversible covalent enzyme inhibitor: X-ray crystallographic analysis of an exceptionally potent α-ketoheterocycle inhibitor of fatty acid amide hydrolase. (2011) (32)
- NMR STUDIES OF CO.DEGLYCOBLEOMYCIN A2 GREEN AND ITS COMPLEX WITH D(CCAGGCCTGG) (1998) (32)
- BINDING-INDUCED ACTIVATION OF DNA ALKYLATION BY DUOCARMYCIN SA: INSIGHTS FROM THE STRUCTURE OF AN INDOLE DERIVATIVE-DNA ADDUCT (1999) (32)
- A novel, unusually efficacious duocarmycin carbamate prodrug that releases no residual byproduct. (2012) (32)
- Arachidonic acid amide inhibitors of gap junction cell-cell communication. (1999) (32)
- MULTISTEP CONVERGENT SOLUTION-PHASE COMBINATORIAL SYNTHESIS AND DELETION SYNTHESIS DECONVOLUTION (1998) (32)
- Probing the role of the vancomycin e-ring aryl chloride: selective divergent synthesis and evaluation of alternatively substituted E-ring analogues. (2013) (32)
- Synthesis and evaluation of a series of C3-substituted CBI analogues of CC-1065 and the duocarmycins. (2001) (32)
- Total synthesis of (+)-camptothecin (2002) (32)
- Synthesis and evaluation of vancomycin aglycon analogues that bear modifications in the N-terminal D-leucyl amino acid. (2009) (32)
- Rational design, synthesis, and evaluation of key analogues of CC-1065 and the duocarmycins. (2007) (32)
- Total synthesis of (.+-.)-N-(phenylsulfonyl)- and (.+-.)-N-(tert-butyloxycarbonyl)-CI, (.+-.)-CI-CDPI1, and (.+-.)-CI-CDPI2: CC-1065 functional analogs incorporating the parent 1,2,7,7a-tetrahydrocycloprop[1,2-c]indol-4-one (CI) left-hand subunit (1989) (32)
- Cytokine receptor dimerization and activation: prospects for small molecule agonists. (2001) (31)
- Chemical and Structural Comparison of N-BOC-CBQ and N-BOC-CBI: Identification and Structural Origin of an Unappreciated but Productive Stability of the CC-1065 and Duocarmycin SA Alkylation Subunits (1994) (31)
- Solution-phase combinatorial synthesis via the olefin metathesis reaction (1997) (31)
- Dissecting ramoplanin: mechanistic analysis of synthetic ramoplanin analogues as a guide to the design of improved antibiotics. (2004) (31)
- Selective metal cation activation of a DNA alkylating agent: synthesis and evaluation of methyl 1,2,9, 9a-Tetrahydrocyclopropa[c]pyrido[3,2-e]indol-4-one-7-carboxylate (CPyI). (2000) (31)
- Discovery of inhibitors of aberrant gene transcription from Libraries of DNA binding molecules: inhibition of LEF-1-mediated gene transcription and oncogenic transformation. (2009) (31)
- A concise synthesis of the fredericamycin A DEF ring system: [4 + 2] cycloaddition reactions of 1-aza-1,3-butadienes (1992) (31)
- The Difference a Single Atom Can Make: Synthesis and Design at the Chemistry–Biology Interface (2017) (31)
- CROSSING EXTREME MECHANISTIC BARRIERS BY ANTIBODY CATALYSIS : SYN ELIMINATION TO A CIS OLEFIN (1994) (31)
- DNA binding properties of key sandramycin analogues: systematic examination of the intercalation chromophore. (1999) (31)
- Cycloadditions of 1,2,3-Triazines Bearing C5-Electron Donating Substituents: Robust Pyrimidine Synthesis. (2015) (30)
- Synthesis and stereochemical determination of complestatin A and B (neuroprotectin A and B). (2011) (30)
- Solution-phase combinatorial synthesis: Convergent multiplication of diversity via the olefin metathesis reaction (1998) (30)
- A Human Single-Chain Antibody Specific for Integrin α3β1 Capable of Cell Internalization and Delivery of Antitumor Agents (2004) (30)
- Synthesis of appropriately functionalized vancomycin CD and DE ring systems (1995) (30)
- Total synthesis of dihydrolysergic acid and dihydrolysergol: development of a divergent synthetic strategy applicable to rapid assembly of D-ring analogs. (2015) (30)
- Rational design of fatty acid amide hydrolase inhibitors that act by covalently bonding to two active site residues. (2013) (30)
- Establishment of substituent effects in the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065. (2003) (30)
- Design, synthesis, and biological evaluation of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase. (2003) (30)
- Synthesis of l,l-isodityrosine (1989) (30)
- α-Ketoheterocycle-based Inhibitors of Fatty Acid Amide Hydrolase (FAAH). (2012) (30)
- TOTAL SYNTHESIS OF GRANDITROPONE, GRANDIRUBRINE, IMERUBRINE, AND ISOIMERUBRINE (1995) (30)
- Pyridine construction via thermal cycloaddition of 1,2,4-triazines with enamines: studies on the preparation of the biaryl CD rings of streptonigrin (1982) (30)
- Establishing the parabolic relationship between reactivity and activity for derivatives and analogues of the duocarmycin and CC-1065 alkylation subunits. (2004) (29)
- Antimicrobial and cytotoxic properties of 9,10-dihydrophenanthrenes: structure-activity studies on juncusol. (1985) (29)
- A Systematic Evaluation of the Bleomycin A2 l-Threonine Side Chain: Its Role in Preorganization of a Compact Conformation Implicated in Sequence-Selective DNA Cleavage (1998) (29)
- Thermal cycloaddition reactions of .pi.-delocalized singlet vinylcarbenes: three-carbon 1,1-/1,3-dipoles. The thermal three-carbon + two-carbon cycloaddition (1988) (29)
- Disruption of the MYC transcriptional function by a small-molecule antagonist of MYC/MAX dimerization. (2008) (29)
- Critical Role of the Linking Amide in CC-1065 and the Duocarmycins: Implications on the Source of DNA Alkylation Catalysis (1998) (29)
- DEFINITION OF THE EFFECT AND ROLE OF THE BLEOMYCIN A2 VALERATE SUBSTITUENTS : PREORGANIZATION OF A RIGID, COMPACT CONFORMATION IMPLICATED IN SEQUENCE- SELECTIVE DNA CLEAVAGE (1998) (29)
- A Novel Class of CC-1065 and Duocarmycin Analogues Subject to Mitomycin-Related Reductive Activation. (1999) (29)
- Insights into the mechanism of streptonigrin-induced protein arginine deiminase inactivation. (2014) (29)
- A simplified isoquinoline synthesis (1981) (29)
- Key Synthetic Analogs of Bleomycin A2 That Directly Address the Effect and Role of the Disaccharide: Demannosylbleomycin A2 and .alpha.-D-Mannopyranosyldeglycobleomycin A2 (1995) (29)
- Inhibitors of cell migration that inhibit intracellular paxillin/alpha4 binding: a well-documented use of positional scanning libraries. (2002) (29)
- Total Synthesis of HUN-7293 (1999) (28)
- Discovery of HIV fusion inhibitors targeting gp41 using a comprehensive α-helix mimetic library. (2012) (28)
- Selectively protected L-dopa derivatives: application of the benzylic hydroperoxide rearrangement (1987) (28)
- Chapter 2 - Recent Applications of the Inverse Electron Demand Diels-Alder Reaction (1989) (28)
- Diprovocims: A New and Exceptionally Potent Class of Toll-like Receptor Agonists. (2018) (28)
- Design, Synthesis, and Evaluation of CC-1065 and Duocarmycin Analogs Incorporating the 2,3,10,10a-Tetrahydro-1H-cyclopropa[d]benzo[f]quinol-5-one (CBQ) Alkylation Subunit: Identification and Structural Origin of Subtle Stereoelectronic Features That Govern Reactivity and Regioselectivity (1994) (28)
- Parallel synthesis and evaluation of 132 (+)-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) analogues of CC-1065 and the duocarmycins defining the contribution of the DNA-binding domain. (2001) (28)
- 1,2,4-triazine preparation via thermal cycloaddition of dimethyl 1,2,4,5-tetrazine-3,6-dicarboxylate with aryl thioimidates (1984) (28)
- Target-Based Screen Against a Periplasmic Serine Protease That Regulates Intrabacterial pH Homeostasis in Mycobacterium tuberculosis (2014) (28)
- Synthesis and preliminary evaluation of (+)-CBI-indole2: an enhanced functional analog of (+)-CC-1065 (1991) (28)
- Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase. (2005) (27)
- Regiocontrolled nucleophilic addition to selectively activated p-quinone diimines: alternative preparation of a key intermediate employed in the preparation of the CC-1065 left-hand subunit (1990) (27)
- Diels-Alder Reactions of Cyclopropenone Ketals: A Concise Tropolone Annulation Applicable to Rubrolone C Ring Introduction (1994) (27)
- 10-Formyl-5,8,10-trideazafolic acid (10-formyl-TDAF): a potent inhibitor of glycinamide ribonucleotide transformylase. (1997) (27)
- Synthesis and evaluation of 1,2,8, 8a-Tetrahydrocyclopropa[c]pyrrolo[3,2-e]indol-4(5H)-one, the parent alkylation subunit of CC-1065 and the duocarmycins: impact of the alkylation subunit substituents and its implications for DNA alkylation catalysis. (2000) (27)
- A Modified Friedlander Condensation for the Synthesis of 3-Hydroxyquinoline-2-carboxylates (1995) (27)
- Solution Phase Combinatorial Synthesis of Biaryl Libraries Employing Heterogeneous Conditions for Catalysis and Isolation with Size Exclusion Chromatography for Purification (1999) (27)
- Crystal structures of human GAR Tfase at low and high pH and with substrate beta-GAR. (2002) (27)
- Synthetic analgesics: preparation of racemic 6,7-benzomorphans (1982) (26)
- Total Synthesis of (−)-Pyrimidoblamic Acid and Deglycobleomycin A2† (1993) (26)
- Alternative Synthesis of the Cycloisodityrosine Subunit of Deoxybouvardin, RA-VII, and Related Agents: Reassignment of the Stereochemistry of Prior Intermediates. (1996) (26)
- CC-1065 partial structures :enhancement of noncovalent affinity for DNA minor groove binding through introduction of stabilizing electrostatic interactions (1992) (26)
- Design, synthesis, and evaluation of duocarmycin O-amino phenol prodrugs subject to tunable reductive activation. (2010) (26)
- Thermal, four-carbon + three-carbon cycloaddition reaction of cyclopropenone ketals. Total synthesis of deacetamidocolchiceine: formal total synthesis of colchicine (1985) (26)
- Effective asymmetric synthesis of 1,2,9,9a-tetrahydrocyclopropa[c]benzo[e]indol-4-one (CBI). (2004) (26)
- Small-Molecule Fusion Inhibitors Bind the pH-Sensing Stable Signal Peptide-GP2 Subunit Interface of the Lassa Virus Envelope Glycoprotein (2016) (26)
- A new and improved method for deglycosidation of glycopeptide antibiotics exemplified with vancomycin, ristocetin, and ramoplanin. (2003) (26)
- Enzymatic Glycosylation of Vancomycin Aglycon: Completion of a Total Synthesis of Vancomycin and N- and C-Terminus Substituent Effects of the Aglycon Substrate (2014) (26)
- Synthesis of Acyclic Precursors to (3S,4S)-4-Hydroxy-2,3,4,5-tetrahydropyridazine-3-carboxylic Acid and Incorporation into a Luzopeptin/Quinoxapeptin Dipeptide. (1998) (26)
- Total synthesis of (+)- and (-)-CPI-CDPI2: (+)-(3bR,4aS)- and (-)-(3bS,4aR)-deoxy-CC-1065 (1988) (26)
- N-Desmethyl Derivatives of Deoxybouvardin and RA-VII: Synthesis and Evaluation (1995) (25)
- Hairpin versus Extended DNA Binding of a Substituted β-Alanine Linked Polyamide (2002) (25)
- Synthesis of key analogs of bleomycin A2 that permit a systematic evaluation of the linker region: identification of an exceptionally prominent role for the L-threonine substituent. (1995) (25)
- Total synthesis and evaluation of phostriecin and key structural analogues. (2010) (24)
- Total synthesis, stereochemical reassignment, and absolute configuration of chlorofusin. (2007) (24)
- Heterocyclic and acyclic azadiene diels‐alder reactions: Total synthesis of nothapodytine B (1998) (24)
- Synthesis of the chlorofusin cyclic peptide: assignment of the asparagine stereochemistry. (2003) (24)
- Characterization of lassa virus cell entry inhibitors: determination of the active enantiomer by asymmetric synthesis. (2009) (24)
- Fe(III)/NaBH4‐Mediated Free Radical Hydrofluorination of Unactivated Alkenes. (2013) (24)
- Asymmetric synthesis of 1,2,9,9a-tetrahydrocyclopropa[c]benzo[e]indol-4-one (CBI). (2011) (24)
- Direct introduction of nitriles via use of unstable Reissert intermediates: convenient procedures for the preparation of 2-cyanoquinolines and 1-cyanoisoquinolines (1984) (24)
- Inhibition of adenovirus replication by a trisubstituted piperazin-2-one derivative. (2014) (23)
- Synthesis of desacetamidopyrimidoblamic acid and deglyco desacetamidobleomycin A2 (1992) (23)
- The structural basis for in situ activation of DNA alkylation by duocarmycin SA. (2000) (23)
- Vancomycin CD and DE Macrocyclization and Atropisomerism Studies. (1999) (23)
- Total synthesis of (-)-and ent-(+)-4 -desacetoxy -5 -desethylvindoline (2007) (23)
- CSI-FID: high throughput label-free detection of DNA binding molecules. (2009) (23)
- SECOND DEFINITIVE TEST OF PROPOSED MODELS FOR THE ORIGIN OF THE CC-1065 AND DUOCARMYCIN DNA ALKYLATION SELECTIVITY (1995) (23)
- Small molecule peptidomimetic inhibitors of importin α/β mediated nuclear transport. (2010) (23)
- Effective, thermal one-carbon + two-carbon cycloaddition of cyclopropenone ketals with electron-deficient olefins: Cyclopropane formation. (1984) (23)
- Singlet oxygen mediated oxidative decarboxylation of pyrrole-2-carboxylic acids (1991) (23)
- Discovery and Structure-Activity Relationships of the Neoseptins: A New Class of Toll-like Receptor-4 (TLR4) Agonists. (2016) (23)
- Synthesis of desacetamido P-3A: 1,3,5-triazine .fwdarw. pyrimidine heteroaromatic azadiene Diels-Alder reaction (1992) (22)
- Synthesis of key sandramycin analogs: systematic examination of the intercalation chromophore. (1998) (22)
- Resveratrol trimer enhances gene delivery to hematopoietic stem cells by reducing antiviral restriction at endosomes. (2019) (22)
- Unexpected Formation of an Epoxide Derived Multisubstrate Adduct Inhibitor on the Active Site of GAR Transformylase (2001) (22)
- Non-Amide-Based Combinatorial Libraries Derived fromN-Boc-Iminodiacetic Acid: Solution-Phase Synthesis of Piperazinone Libraries with Activity Against LEF-1/β-Catenin-Mediated Transcription (2000) (22)
- Design, synthesis, and evaluation of DNA minor groove binding agents: the duocarmycins (1994) (22)
- Are the Duocarmycin and CC-1065 DNA Alkylation Reactions Acid-Catalyzed? Solvolysis pH-Rate Profiles Suggest They Are Not. (1999) (22)
- Synthesis and evaluation of selected key methyl ether derivatives of vancomycin aglycon. (2010) (22)
- Total Synthesis and Stereochemical Assignment of Streptide. (2019) (22)
- Hypervalent iodine(III)-promoted intermolecular C-C coupling of vindoline with β-ketoesters and related substrates. (2013) (22)
- Synthesis and evaluation of methyl ether derivatives of the vancomycin, teicoplanin, and ristocetin aglycon methyl esters. (2003) (22)
- Total synthesis of (-)-kopsinine and ent-(+)-kopsinine. (2015) (21)
- High-resolution assessment of protein DNA binding affinity and selectivity utilizing a fluorescent intercalator displacement (FID) assay. (2003) (21)
- Intramolecular [1 + 2] and [3 + 2] cycloaddition reactions of cyclopropenone ketals. (2010) (21)
- CBI Prodrug Analogs of CC-1065 and the Duocarmycins (1999) (21)
- Maxamycins: Durable Antibiotics Derived by Rational Redesign of Vancomycin. (2020) (21)
- CBI-CDPBO1 and CBI-CDPBI1: CC-1065 analogs containing deep-seated modifications in the DNA binding subunit. (1995) (21)
- New annulation processes for fused and spiro rings based on the chemistry of benzothiazoles (1978) (21)
- Studies on the total synthesis of fredericamycin A: Development of an intermolecular alkyne-chromium carbene complex cyclization approach to the ABCDE ring system (1989) (21)
- Identification of broad-based HIV-1 protease inhibitors from combinatorial libraries. (2010) (21)
- Solution-phase synthesis of combinatorial libraries designed to modulate protein-protein or protein-DNA interactions. (2003) (21)
- Synthesis, characterization, and cycloaddition reactivity of a monocyclic aromatic 1,2,3,5-tetrazine. (2019) (20)
- Design, Synthesis, and Characterization of α-Ketoheterocycles That Additionally Target the Cytosolic Port Cys269 of Fatty Acid Amide Hydrolase (2014) (20)
- DNA Alkylation Properties of CC-1065 and Duocarmycin Analogs Incorporating the 2,3,10,10a-Tetrahydrocyclopropa[d]benzo[f]quinol-5-one Alkylation Subunit: Identification of Subtle Structural Features That Contribute to the Regioselectivity of the Adenine N3 Alkylation Reaction (1995) (20)
- Total synthesis, assignment of the relative and absolute stereochemistry, and structural reassignment of phostriecin (aka Sultriecin). (2010) (20)
- Functional and biochemical analysis of a key series of ramoplanin analogues. (2009) (20)
- An unusually facile SnAr 14-membered biaryl ether macrocyclization reaction suitable for preparation of the cycloisodityrosine subunit of bouvardin, deoxybouvardin and related agents (1995) (20)
- Development of a solution-phase synthesis of minor groove binding bis-intercalators based on triostin A suitable for combinatorial synthesis. (2000) (20)
- Applications of Free Radicals in Organic Synthesis (1997) (19)
- An additional spirocyclization for duocarmycin SA. (2008) (19)
- Convergent Solution-Phase Combinatorial Synthesis with Multiplication of Diversity through Rigid Biaryl and Diarylacetylene Couplings (1999) (19)
- Assessment of solution-phase positional scanning libraries based on distamycin A for the discovery of new DNA binding agents. (2000) (19)
- Next-Generation Total Synthesis of Vancomycin. (2020) (19)
- Functionalized analogues of 5,8,10-trideazafolate: development of an enzyme-assembled tight binding inhibitor of GAR Tfase and a potential irreversible inhibitor of AICAR Tfase. (1997) (19)
- Generation of targeted C2-symmetrical compound libraries by solution-phase combinatorial chemistry (1997) (19)
- Higher order iminodiacetic acid libraries for probing protein-protein interactions. (1998) (19)
- A potent, simple derivative of an analog of the CC-1065 alkylation subunit (1991) (19)
- Benzylic hydroperoxide rearrangement: observations on a viable and convenient alternative to the Baeyer-Villiger rearrangement (1986) (19)
- Discovery of small-molecule enzyme activators by activity-based protein profiling (2020) (19)
- Thermal atropisomerism of fully functionalized vancomycin CD, DE, and CDE ring systems (1997) (19)
- Vancomycin C-Terminus Guanidine Modifications and Further Insights into an Added Mechanism of Action Imparted by a Peripheral Structural Modification. (2020) (19)
- Oxidative coupling of methyl 6-hydroxyindole-2-carboxylate with primary amines. Preparation of 2-substituted methyl pyrrolo[2,3-e]benzoxazole-5-carboxylates (1988) (19)
- Diels-Alder Reactions of Heterocyclic Azadienes: Scope and Applications (1987) (18)
- Design, synthesis and evaluation of bouvardin, deoxybouvardin and RA-I-XIV pharmacophore analogs. (1994) (18)
- A new class of highly cytotoxic diketopiperazines. (2000) (18)
- Synthesis of tri- and tetrapeptide S: the extended C-terminus of bleomycin A2 (1992) (18)
- Functionalized analogues of 5,8,10-trideazafolate as potential inhibitors of GAR Tfase or AICAR Tfase. (1997) (18)
- Asymmetric Synthesis of the CBI Alkylation Subunit of the CC-1065 and Duocarmycin Analogs (1997) (18)
- Synthesis of N29-desmethyl RA-VII. Identification of the pharmacophore of RA-I-VII and deoxybouvardin and reassignment of the subunit functional roles (1992) (18)
- Ultrapotent vinblastines in which added molecular complexity further disrupts the target tubulin dimer–dimer interface (2016) (18)
- N-Terminus Alkylation of Vancomycin: Ligand Binding Affinity, Antimicrobial Activity, and Site-Specific Nature of Quaternary Trimethylammonium Salt Modification. (2018) (18)
- Synthesis of isochrysohermidin-distamycin hybrids. (2003) (18)
- Evaluation of functional analogs of CC-1065 and the duocarmycins incorporating the cross-linking 9a-chloromethyl-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-on e (C2BI) alkylation subunit. (1993) (18)
- 10-Formyl-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid (10-formyl-DDACTHF): a potent cytotoxic agent acting by selective inhibition of human GAR Tfase and the de novo purine biosynthetic pathway. (2002) (18)
- Synthesis and evaluation of vancomycin and vancomycin aglycon analogues that bear modifications in the residue 3 asparagine. (2002) (18)
- Design, synthesis, and evaluation of DNA minor groove binding agents (1993) (17)
- Studies on the synthesis of rubrolone: 4π participation of O-alkyl α,β-unsaturated oximes in intramolecular [4 + 2] cycloaddition reactions (1991) (17)
- A Hammett correlation for CC-1065 and duocarmycin analogs: magnitude of substituent electronic effects on functional reactivity. (1996) (17)
- Assessment of the Role of the Bleomycin A2 Pyrimidoblamic Acid C4 Amino Group (1998) (17)
- Mechanisms of in situ Activation for DNA-Targeting Antitumor Agents (2002) (17)
- Preparation of the 14-membered l,l-cycloisodityrosine subunit of RP 66453 (2002) (17)
- Indole N-carbonyl compounds: preparation and coupling of indole-1-carboxylic acid anhydride (1987) (17)
- Structure-based Design, Synthesis, Evaluation, and Crystal Structures of Transition State Analogue Inhibitors of Inosine Monophosphate Cyclohydrolase* (2007) (17)
- Synthesis of (9S,12S)-cycloisodityrosine and its unnatural (9R,12S)-diastereomer (1996) (17)
- A study of the scope of the [4 + 2] cycloaddition reactions of unactivated 1,3-oxazin-6-ones (1989) (17)
- Thermal Atropisomerism of Teicoplanin Aglycon Derivatives: Preparation of the P,P,P and M,P,P Atropisomers of the Teicoplanin Aglycon via Selective Equilibration of the DE Ring System (2000) (17)
- Preparation of optically active, functionalized cis-.DELTA.6-1-octalones (1985) (16)
- Application of benzothiazoles to carbon-carbon bond formation in organic synthesis (1978) (16)
- Key analogs of the tetrapeptide subunit of RA-VII and deoxybouvardin. (1995) (16)
- Efficacious cyclic N-acyl O-amino phenol duocarmycin prodrugs. (2013) (16)
- Demonstration and definition of the noncovalent binding selectivity of agents related to CC-1065 by an affinity cleavage agent: noncovalent binding coincidental with alkylation. (1996) (16)
- Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization. (2005) (16)
- Synthesis and evaluation of deglycobleomycin A2 analogues containing a tertiary N-methyl amide and simple ester replacement for the L-histidine secondary amide: direct functional characterization of the requirement for secondary amide metal complexation. (1996) (16)
- Design of Benzoxathiazin-3-one 1,1-Dioxides as a New Class of Irreversible Serine Hydrolase Inhibitors: Discovery of a Uniquely Selective PNPLA4 Inhibitor. (2017) (16)
- Synthesis and Evaluation of Duocarmycin and CC-1065 Analogues Containing Modifications in the Subunit Linking Amide. (1999) (16)
- Activation and coupling of pyrrole-1-carboxylic acid in the formation of pyrrole N-carbonyl compounds: pyrrole-1-carboxylic acid anhydride (1987) (16)
- Determination of binding affinities of triplex forming oligonucleotides using a fluorescent intercalator displacement (FID) assay. (2003) (16)
- Design, synthesis and biological evaluation of 10-CF3CO-DDACTHF analogues and derivatives as inhibitors of GAR Tfase and the de novo purine biosynthetic pathway. (2003) (15)
- Synthesis of the vancomycin CDE ring system. (1998) (15)
- Investigation into the functional impact of the vancomycin C-ring aryl chloride. (2013) (15)
- The DNA phosphate backbone is not involved in catalysis of the duocarmycin and CC-1065 DNA alkylation reaction. (2002) (15)
- Unexpected formation of an epoxide-derived multisubstrate adduct inhibitor on the active site of GAR transformylase. (2001) (15)
- Metal cation complexation and activation of reversed CPyI analogues of CC-1065 and duocarmycin SA: partitioning the effects of binding and catalysis. (2001) (15)
- Design, synthesis, and evaluation of potential GAR and AICAR transformylase inhibitors. (1998) (15)
- Preparation of (R)-(+)- and (S)-(-)-4-iodo-1,2-epoxybutane [(R)- and (S)-(2-iodoethyl)oxirane], useful chiral synthons (1981) (15)
- Abenzyl 10-formyl-trideazafolic acid (abenzyl 10-formyl-TDAF): an effective inhibitor of glycinamide ribonucleotide transformylase. (1997) (15)
- (-)-Sandramycin : total synthesis and preliminary DNA binding properties (1993) (15)
- Comprehensive high-resolution analysis of hairpin polyamides utilizing a fluorescent intercalator displacement (FID) assay. (2003) (14)
- A fundamental relationship between hydrophobic properties and biological activity for the duocarmycin class of DNA-alkylating antitumor drugs: hydrophobic-binding-driven bonding. (2013) (14)
- CC-1065 CBI analogs: an example of enhancement of DNA alkylation efficiency through introduction of stabilizing electrostatic interactions. (1995) (14)
- Higher order iminodiacetic acid libraries for probing protein-protein interactions. (1998) (14)
- Synthesis and evaluation of N-aryl and N-alkenyl CBI derivatives. (2004) (14)
- Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase. (2000) (14)
- Synthesis and DNA binding properties of iminodiacetic acid-linked polyamides: characterization of cooperative extended 2:1 side-by-side parallel binding. (2002) (14)
- Selective N1/N4 1,4-Cycloaddition of 1,2,4,5-Tetrazines Enabled by Solvent Hydrogen Bonding. (2020) (14)
- A new and unusually flexible scheme for annulatton to form fused cyclohexenone units (1978) (14)
- A comparative study of the solvolysis reactivity, regioselectivity, and stereochemistry of the duocarmycin a and sa alkylation subunits (1996) (14)
- Synthesis and Evaluation of the Fully Functionalized Bleomycin A2 Metal Binding Domain Containing the 2-O-(3-O-Carbamoyl-.alpha.-D-mannopyranosyl)-.alpha.-L-gulopyranosyl Disaccharide (1995) (14)
- Inverse electron demand diels-alder reaction of 3-carbomethoxy-2-pyrones with 1,1-dimethoxyethylene: a simple and mild method of aryl annulation (1982) (14)
- Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. (2007) (14)
- Solution Phase Conformational Studies of the Cyclic Peptide RA-VII: Lithium Chloride Perturbation of the Conformational Equilibria (1995) (13)
- Deglyco GABA-Gly-desacetamidobleomycin A2: a simplified synthetic model for bleomycin A2 (1992) (13)
- Vinblastine 20' Amides: Synthetic Analogues That Maintain or Improve Potency and Simultaneously Overcome Pgp-Derived Efflux and Resistance. (2017) (13)
- Multisubstrate analogue based on 5,8,10-trideazafolate. (1997) (13)
- Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase. (2007) (13)
- Identification of Small Mole (2007) (13)
- Comprehensive Analysis of Structure-Activity Relationships of α-Ketoheterocycles as sn-1-Diacylglycerol Lipase α Inhibitors. (2015) (13)
- Resolution of a CPzI precursor, synthesis and biological evaluation of (+) and (-)-N-Boc-CPzI: a further validation of the relationship between chemical solvolytic stability and cytotoxicity. (1999) (13)
- Examination of the role of the duocarmycin SA methoxy substituents: Identification of the minimum, fully potent DNA binding subunit (1996) (13)
- Streptonigrin and lavendamycin partial structures. Preparation of 7-amino-2-(2′-pyridyl)quinoline-5,8-quinone-6′-carboxylic acid: A probe for the minimum, potent pharmacophore of the naturally occurring antitumor-antibiotics (1987) (13)
- Total Syntheses of Thiocoraline and BE-22179: Establishment of Relative and Absolute Stereochemistry. (2000) (13)
- Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase. (2008) (13)
- p-Quinonemethide analog of the CC-1065 and duocarmycin alkylation subunits (1994) (13)
- C1-CBP-vancomycin: Impact of a Vancomycin C-Terminus Trimethylammonium Cation on Pharmacological Properties and Insights into Its Newly Introduced Mechanism of Action. (2019) (13)
- Synthesis and evaluation of a thio analogue of duocarmycin SA. (2009) (13)
- Inverse electron demand diels-alder reactions of 3-carbomethoxy-2-pyrones. Controlled introduction of oxygenated aromatics: benzene, phenol, catechol, resorcinol, pyrogallol annulation. (1983) (13)
- Synthesis, Characterization, and Rapid Cycloadditions of 5-Nitro-1,2,3-triazine. (2018) (12)
- CC‐1065 and the Duocarmycins: Understanding Their Biological Function Through Mechanistic Studies (1996) (12)
- Divergent Total Syntheses of (-)-Pseudocopsinine and (-)-Minovincinine. (2020) (12)
- Glycinamide ribonucleotide transformylase (GAR Tfase) as a target for cancer therapy (2008) (12)
- Total synthesis of a key series of vinblastines modified at C4 that define the importance and surprising trends in activity (2016) (12)
- Direct Synthesis of β-Aminoenals through Reaction of 1,2,3-Triazine with Secondary Amines. (2017) (12)
- Precise Targeted Cleavage of a r(CUG) Repeat Expansion in Cells by Using a Small-Molecule-Deglycobleomycin Conjugate. (2020) (12)
- Energetic preferences for alpha,beta versus beta,gamma unsaturation. (2004) (12)
- A New Method of in Situ Activation for a Novel Class of DNA Alkylating Agents: Tunable Metal Cation Complexation and Activation (2000) (12)
- Intramolecular Diels-Alder reactions of cyclopropenone ketals. (2010) (12)
- Vancomycin, Teicoplanin, and Ramoplanin: Synthetic and Mechanistic Studies (2001) (12)
- Inverse Electron Demand Diels-Alder Reactions of Heterocyclic Aza Dienes. (1986) (12)
- Synthesis and DNA binding properties of saturated distamycin analogues. (2002) (12)
- Further observations on the Lewis acid-catalyzed benzylic hydroperoxide rearrangement: use of a boron-trifluoride/ hydrogen peroxide preformed, aged reagent (1987) (11)
- pH Dependence of the rate of DNA alkylation for (+)-duocarmycin SA and (+)-CCBI-TMI (1997) (11)
- Synthesis and evaluation of aza HUN-7293. (2000) (11)
- N-Acyl pyrazoles: Effective and tunable inhibitors of serine hydrolases. (2019) (11)
- Synthesis of the (S,S,S)-diastereomer of the 15-membered biaryl ring system of RP 66453 (2003) (11)
- Total Synthesis of HUN-7293. (1999) (11)
- Thermal, three-carbon + two-atom cycloaddition of cyclopropenone ketals with carbon-heteroatom double bonds: Butenolide, furan, and γ-keto ester preparation. (1984) (11)
- FAAH inhibitor OL-135 disrupts contextual, but not auditory, fear conditioning in rats (2016) (10)
- Synthesis and evaluation of duocarmycin and CC-1065 analogues incorporating the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]-3-azaindol-4-one (CBA) alkylation subunit. (2003) (10)
- Total Synthesis of (-)-Strempeliopine. (2021) (10)
- Optimization and characterization of a pan protein arginine deiminase (PAD) inhibitor (2013) (10)
- Chemistry and Biology of Ramoplanin: A Lipoglycodepsipeptide with Potent Antibiotic Activity (2005) (10)
- Substituent effects within the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065. (2001) (10)
- Regioselectivity in the intermolecular Diels-Alder reaction of acyl nitroso compounds (C-nitrosocarbonyl compounds) and nitrosoformates (O-nitrosocarbonyl compounds) (1984) (9)
- Total Synthesis of Vinblastine, Related Natural Products, and Key Analogues and Development of Inspired Methodology Suitable for the Systematic Study of Their Structure‐Function Properties (2015) (9)
- Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase. (2006) (9)
- Synthesis and evaluation of duocarmycin SA analogs incorporating the methyl 1,2,8,8a-tetrahydrocyclopropa[c]oxazolo[2,3-e]indol-4-one-6-carboxylate (COI) alkylation subunit. (2010) (9)
- alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: carbonyl group modification and alpha-substitution. (2001) (9)
- A simple and convenient phenol annulation (1980) (9)
- Triarylaminium Radical Cation Promoted Coupling of Catharanthine with Vindoline: Diastereospecific Synthesis of Anhydrovinblastine and Reaction Scope. (2019) (9)
- Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase. (2000) (9)
- Key analogs of a uniquely potent synthetic vinblastine that contain modifications of the C20' ethyl substituent. (2017) (9)
- An improved and divergent introduction of the streptonigrin and lavendamycin quinoline 5 8 quinone ab ring systems (1986) (9)
- Duocarmycin-Pyrindamycin DNA Alkylation Properties and Identification, Synthesis, and Evaluation of Agents Incorporating the Pharmacophore of the Duocarmycin-Pyrindamycin Alkylation Subunit. Identification of the CC-1065-Duocarmycin Common Pharmacophore. (1991) (9)
- Evaluation of a reductively activated duocarmycin prodrug against murine and human solid cancers (2013) (9)
- The quest for supernatural products: the impact of total synthesis in complex natural products medicinal chemistry. (2020) (9)
- Correlation of inhibitor effects on enzyme activity and thermal stability for the integral membrane protein fatty acid amide hydrolase. (2008) (9)
- Total Synthesis of Bouvardin, O-Methylbouvardin, and O-Methyl-N9- desmethylbouvardin. (1995) (9)
- CC-1065/duocarmycin and bleomycin A2 hybrid agents: lack of enhancement of DNA alkylation by attachment to noncomplementary DNA binding subunits. (1997) (8)
- A human single-chain antibody specific for integrin alpha3beta1 capable of cell internalization and delivery of antitumor agents. (2004) (8)
- Evaluation of Chlorofusin, its Seven Chromophore Diastereomers, and Key Analogues. (2009) (8)
- Evaluation of bouvardin, deoxybouvardin, and RA-I - RA-VII partial structures: reassignment of the pharmacophore (1991) (8)
- Asymmetric Synthesis of a CBI-Based Cyclic N-Acyl O-Amino Phenol Duocarmycin Prodrug (2014) (8)
- Bifunctional alkylating agents derived from duocarmycin SA: potent antitumor activity with altered sequence selectivity. (2000) (8)
- Thermal Atropisomerism of Teicoplanin Aglycon Derivatives. Preparation of the P,P,P and M,P,P Atropisomers of the Teicoplanin Aglycon via Selective Equilibration of the DE Ring System. (2001) (8)
- Preparation of 3‐methyl‐4‐vinyl‐1,2,5‐oxadiazole and 3‐methyl‐4‐vinyl‐1,2,5‐thiadiazole (1981) (8)
- An exceptionally potent analog of sandramycin (1997) (8)
- Acyl Radicals: Intermolecular and Intramolecular Alkene Addition Reactions. (1992) (8)
- Synthesis and evaluation of a series of C5'-substituted duocarmycin SA analogs. (2010) (8)
- Synthesis and X-ray analysis of an unprecedented and stable 2-aza-4,4-spirocyclopropacyclohexadienone. (2003) (8)
- Total synthesis of OF4949-III and OF4949-IV: Unusual effects of remote substituents on the rate of macrocyclization reactions (1989) (8)
- N-methyl threonine analogues of deglycobleomycin A2: synthesis and evaluation. (1997) (8)
- Discovery libraries targeting the major enzyme classes: the serine hydrolases. (2014) (8)
- Diastereoselective Total Synthesis of the Vancomycin Aglycon with Ordered Atropisomer Equilibrations. (1999) (8)
- Synthesis and Preliminary Evaluation of Duocarmycin Analogues Incorporating the 1,2,11,11a-Tetrahydrocyclopropa[c]naphtho[2,3-e]indol-4-one (CNI) and 1,2,11,11a-Tetrahydrocyclopropa[c]naphtho[1,2-e]indol-4-one (iso-CNI) Alkylation Subunits. (2009) (8)
- A simple method for the purification and isolation of bleomycin A2 (1992) (8)
- Diels-Alder cycloadditions of rigid dienophiles: a probe for allylic axial substituent control of the pi-facial selectivity in the Diels-Alder reaction (1986) (8)
- Synthesis and evaluation of a novel bleomycin A2 analogue: continuing assessment of the linker domain (2000) (7)
- Studies on the synthesis of bleomycin A2 : observations on a diastereoselective imine addition reaction for C2-acetamido side chain introduction (1993) (7)
- Yatakemycin: Total Synthesis, DNA Alkylation, and Biological Properties (2008) (7)
- Synthesis and characterization of a cyclobutane duocarmycin derivative incorporating the 1,2,10,11-tetrahydro-9H-cyclobuta[c]benzo[e]indol-4-one (CbBI) alkylation subunit. (2010) (7)
- Synthesis and evaluation of potential Nπ and Nσ metal chelation sites within the β-hydroxy-l-histidine subunit of bleomycin A2: Functional characterization of imidazole Nπ metal complexation (1996) (7)
- Synthesis and biological evaluation of N-[4-[5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoroacetyl)pentyl]benzoyl]-L-glutamic acid as a potential inhibitor of GAR Tfase and the de novo purine biosynthetic pathway. (2005) (7)
- Biological and structural evaluation of 10R- and 10S-methylthio-DDACTHF reveals a new role for sulfur in inhibition of glycinamide ribonucleotide transformylase. (2013) (7)
- α-Ketoheterocycle inhibitors of fatty acid amide hydrolase: exploration of conformational constraints in the acyl side chain. (2014) (7)
- α‐Keto Heterocycle Inhibitors of Fatty Acid Amide Hydrolase: Carbonyl Group Modification and α‐Substitution. (2001) (7)
- DIELS‐ALDER REACTION OF HETEROCYCLIC AZADIENES. I. THERMAL CYCLOADDITION OF 1,2,4‐TRIAZINE WITH ENAMINES: SIMPLE PREPARATION OF SUBSTITUTED PYRIDINES (2002) (7)
- Exploration of the site-specific nature and generalizability of a trimethylammonium salt modification on vancomycin: A-ring derivatives. (2019) (7)
- Inverse Electron Demand Diels-Alder Reactions of N-Sulfonyl α,. beta.-Unsaturated Imines: A General Approach to Implementation of the 4π Participation of 1-Aza-1,3-butadienes in Diels-Alder Reactions. (1991) (7)
- A powerful selection assay for mixture libraries of DNA alkylating agents. (2004) (6)
- Convergent Solution-Phase Combinatorial Synthesis with Multiplication of Diversity Through Rigid Biaryl and Diarylacetylene Couplings. (2000) (6)
- Total Synthesis and Preliminary Evaluation of (+)‐ and ent‐(‐)‐ Duocarmycin SA. (1994) (6)
- Total Synthesis of Phomazarin. (1999) (6)
- Diels-alder Reactions of Azadienes: Scope and Applications (2010) (6)
- Design and Total Synthesis of a Conformational Analog of Bouvardin/Deoxybouvardin (1990) (6)
- Novel Solution Phase Strategy for the Synthesis of Chemical Libraries Containing Small Organic Molecules. (1996) (6)
- Design, synthesis, and biological evaluation of 10-methanesulfonyl-DDACTHF, 10-methanesulfonyl-5-DACTHF, and 10-methylthio-DDACTHF as potent inhibitors of GAR Tfase and the de novo purine biosynthetic pathway. (2005) (6)
- Diastereoselective Dieckmann condensation suitable for introduction of the duocarmycin A C6 center: development of a divergent strategy for the total synthesis of duocarmycins A and SA. (1995) (6)
- PALLADIUM(0)-MEDIATED β-CARBOLINE SYNTHESIS: PREPARATION OF THE CDE RING SYSTEM OF LAVENDAMYCIN (1984) (6)
- High expression of class III β-tubulin has no impact on functional cancer cell growth inhibition of a series of key vinblastine analogs. (2018) (6)
- K-13 and of4949: Evaluation of key partial structures and pharmacophore delineation (1993) (6)
- P-3A and (−)-desacetamido P-3A: demonstration and Study of their effective functional cleavage of duplex DNA (1992) (6)
- NMR-assisted computational studies of peptidomimetic inhibitors bound in the hydrophobic pocket of HIV-1 glycoprotein 41 (2013) (5)
- A Systematic Evaluation of the Bleomycin A2 L‐Threonine Side Chain: Its Role in Preorganization of a Compact Conformation Implicated in Sequence‐Selective DNA Cleavage. (1999) (5)
- Reversed and Sandwiched Analogues of Duocarmycin SA: Establishment of the Origin of the Sequence-Selective Alkylation of DNA and New Insights into the Source of Catalysis (1997) (5)
- Alternative synthesis and thermal atropisomerism of a fully functionalized DEFG ring system of teicoplanin (2001) (5)
- Inverse Electron Demand Diels-Alder Reactions of 3,6-Bis(methylthio)-1,2,4,5-tetrazine: 1,2-Diazine Introduction and Direct Implementation of a Divergent 1,2,4,5-Tetrazine → 1,2-Diazine → Benzene (Indoline/Indole) Diels-Alder Strategy (1988) (5)
- Synthesis and biological evaluation of alpha- and gamma-carboxamide derivatives of 10-CF3CO-DDACTHF. (2005) (5)
- Vancomycin Aglycon : Reengineering Vancomycin for Dual DAla-DAla and DAla-D-Lac Binding (5)
- Asymmetric Total Synthesis of ent‐(‐)‐Roseophilin: Assignment of Absolute Configuration. (2001) (5)
- d,l- and meso-Isochrysohermidin: Total Synthesis and Interstrand DNA Cross-Linking. (1994) (5)
- Synthesis of the Chlorofusin Cyclic Peptide. (2009) (5)
- Preparation and Diels‐Alder Reaction of a Reactive, Electron‐Deficient Heterocyclic Azadiene: Dimethyl 1,2,4,5‐Tetrazine‐3,6‐Dicarboxylate. 1,2‐Diazine (Dimethyl 4‐Phenyl‐1,2‐Diazine‐3,6‐Dicarboxylate) and Pyrrole (Dimethyl 3‐Phenylpyrrole‐2,5‐Dicarboxylate) Introduction (2003) (5)
- Total Synthesis of Ningalin B Utilizing a Heterocyclic Azadiene Diels—Alder Reaction and Discovery of a New Class of Potent Multidrug Resistant (MDR) Reversal Agents. (2000) (5)
- Total Synthesis of (+)-Piperazinomycin. (1994) (5)
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- Total Synthesis of Bleomycin A2 and Related Agents. Part 4. Synthesis of the Disaccharide Subunit: 2-O-(3-O-Carbamoyl-α-D- mannopyranosyl)-L-gulopyranose and Completion of the Total Synthesis of Bleomycin A2. (1994) (5)
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- REGIOSELECTIVITY OF THE INTERMOLECULAR DIELS‐ALDER REACTION OF ACYL NITROSO COMPOUNDS (C‐NITROSOCARBONYL COMPOUNDS) AND NITROSOFORMATES (O‐NITROSOCARBONYL COMPOUNDS). PREPARATION OF FUNCTIONALIZED CIS‐Δ6‐1‐OCTALONES (1985) (4)
- Total Synthesis and Evaluation of Cytostatin, Its C10—C11 Diastereomers, and Additional Key Analogues: Impact on PP2A Inhibition. (2007) (4)
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- Synthesis and Evaluation of CC‐1065 and Duocarmycin Analogues Incorporating the 1,2,3,4,11,11a‐Hexahydrocyclopropa[c]naphtho[2,1‐b]azepin‐6‐one (CNA) Alkylation Subunit: Structural Features that Govern Reactivity and Reaction Regioselectivity. (1998) (3)
- PREPARATION OF (R)-(+)- AND (S)-(-)-4-IODO-1,2-EPOXYBUTANE ((R)- AND (S)-(2-IODOETHYL)OXIRANE), USEFUL CHIRAL SYNTHONS (1981) (3)
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- Definition of the Effect and Role of the Bleomycin A2 Valerate Substituents: Preorganization of a Rigid, Compact Conformation Implicated in Sequence-Selective DNA Cleavage. (1999) (3)
- Total Synthesis and Evaluation of (.+-.)-N-(tert.-Butyloxycarbonyl)-CBI, (.+-.)-CBI-CDPI1, and (.+-.)-CBI-CDPI2: CC-1065 Functional Agents Incorporating the Equivalent 1,2,9,9a-Tetrahydrocycloprop(1,2-c)benz(1,2-e)indol-4-one (CBI) Le (1989) (3)
- Synthesis of (R)‐(4‐Methoxy‐3,5‐dihydroxyphenyl)glycine Derivatives: The Central Amino Acid of Vancomycin and Related Agents. (1996) (3)
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- Total Synthesis of Bleomycin A2 and Related Agents. Part 3. Synthesis and Comparative Evaluation of Deglycobleomycin A2, Epideglycobleomycin A2, Deglycobleomycin A1, and Desacetamido‐, Descarboxamido‐, Desmethyl‐ , and Desimidazolyldeglycobleomycin A2. (1994) (2)
- Mechanistic Insights into the Reaction of Amidines with 1,2,3-Triazines and 1,2,3,5-Tetrazines (2022) (2)
- Total synthesis of natural (+)- [corrected] and ent-(-)-4-desacetoxy-6,7-dihydrovindorosine [corrected] and natural and ent-minovine: oxadiazole tandem intramolecular Diels-Alder/1,3-dipolar cycloaddition reaction. (2005) (2)
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- Diels-Alder Reactions of 1-Aza-1,3-butadienes: Room Temperature, endo- Selective LUMOdiene-Controlled (4 + 2)Cycloaddition Reactions of N- Sulfonyl-4-(ethoxycarbonyl)-1-aza-1,3-butadienes (I). (1991) (2)
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- Synthesis of N-(tert-butyloxycarbonyl)-CBI, CBI, CBI-CDPI1, and CBI-CDPI2: enhanced functional analogs of CC-1065 incorporating the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) left-hand subunit [Erratum to document cited in CA113(23):211667n] (1991) (1)
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- Synthesis, X‐Ray Structure, and Properties of Fluorocyclopropane Analogues of the Duocarmycins Incorporating the 9,9‐Difluoro‐1,2,9,9a‐ tetrahydrocyclopropa(c)benzo(e)indol‐4‐one (F2CBI) Alkylation Subunit. (1997) (1)
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- An Unusually Facile SNAr 14‐Membered Biaryl Ether Macrocyclization Reaction Suitable for Preparation of the Cycloisodityrosine Subunit of Bouvardin, Deoxybouvardin and Related Agents. (1995) (1)
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- Thermal, Four-Carbon and Three-Carbon Cycloaddition Reaction of Cyclopropenone Ketals. (1986) (0)
- crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase (2006) (0)
- Figure 2, Preparation of coupling partners A and B (2013) (0)
- Cyclopropene, 3,3‐Dimethoxy (2004) (0)
- Intramolecular Acyl Radical-Alkene Addition Reactions: Macrocyclization Reactions. (1990) (0)
- Total Synthesis of Cycloisodityrosine, RA-VII, Deoxybouvardin, and N29- Desmethyl-RA-VII: Identification of the Pharmacophore and Reversal of the Subunit Functional Roles. (1993) (0)
- Symposia-in-printCombinatorial chemistry (1998) (0)
- CCDC 295590: Experimental Crystal Structure Determination (2006) (0)
- Synthesis of Chloropeptin II (2010) (0)
- Total Synthesis of Kopsinine (I). (2013) (0)
- Accelerated Inverse Electron Demand Diels‐Alder Reactions of 1‐Oxa‐1,3‐butadienes: (4 + 2)Cycloaddition Reactions of β,γ‐Unsaturated α‐Keto Esters. (1988) (0)
- NEW ANNULATION FOR FUSED AND SPIRO RINGS BASED ON THE CHEMISTRY OF BENZOTHIAZOLES (1978) (0)
- Total Syntheses of (+)-P-3A (Ia), epi-(-)-P-3A (Ib), and (-)- Desacetamido P-3A (Ic). (2010) (0)
- Acyl Radicals: Functionalized Free Radicals for Intramolecuar Cyclization Reactions. (1988) (0)
- 4-Methyl-1,2,3-triazine† (2001) (0)
- Figure 3, IC50 curves for PADs 1–4 with ML325 (SID 118043677) as determined by biochemical substrate assay using the N-α-benzoyl-L-arginine ethyl ester HCl (BAEE) reagent (2013) (0)
- Total Synthesis of (-)-Pyrimidoblamic Acid and Deglycobleomycin A2. (1993) (0)
- Synthesis and evaluation of potential N pi and N sigma metal chelation sites within the beta-hydroxy-L-histidine subunit of bleomycin A2: functional characterization of imidazole N pi metal complexation. (1996) (0)
- SYNTHETIC ANALGESICS: PREPARATION OF RACEMIC 6,7‐BENZOMORPHANS (1983) (0)
- Bleomycin: Synthetic and Mechanistic Studies (1999) (0)
- Thermal Reactions of Cyclopropenone Ketals. Application of the Cycloaddition Reactions of Delocalized Singlet Vinylcarbenes: Three-Carbon 1,1-/1,3-Dipoles. An Alternative Synthesis of Deacetamidocolchiceine: Formal Total Synthesis of (1987) (0)
- Total Synthesis of (+)- and (-)-CPI-CDPI2: (+)-(3bR,4aS)- and (-)-(3bS,4aR)-Deoxy-CC-1065. (1988) (0)
- An Exceptionally Potent Analogue of Sandramycin. (1997) (0)
- A NEW AND UNUSUALLY FLEXIBLE SCHEME FOR ANNULATION TO FORM FUSED CYCLOHEXENONE UNITS (1979) (0)
- Total Synthesis of (‐)‐ (III) and ent‐(+)‐Vindorosine: Tandem Intramolecular Diels—Alder/1,3‐Dipolar Cycloaddition of 1,3,4‐Oxadiazoles. (2006) (0)
- Diels-Alder Cycloaddition Reactions of Cyclopropenone Ketals. Dual Participation in Inverse Electron Demand (LUMO Controlled) and Normal (HOMO Controlled) Diels-Alder Reactions. (1986) (0)
- Triethyl 1,2,4‐Triazine‐3,5,6‐tricarboxylate (2001) (0)
- Benzylic Hydroperoxide Rearrangement: Observations on a Viable and Convenient Alternative to the Baeyer-Villiger Rearrangement. (1987) (0)
- Singlet Oxygen Oxidation of Bipyrroles: Total Synthesis of d,l‐ and meso‐Isochrysohermidin. (1994) (0)
- Synthesis of Ningalin D (2006) (0)
- High resolution structure of human glycinamide ribonucleotide transformylase in apo form. (2013) (0)
- The crystal structure of mouse TLR4/MD-2/lipid A complex (2016) (0)
- Streptonigrin and Lavendamycin Partial Structures. Preparation of 7-Amino-2-(2′-pyridyl)quinoline-5,8-quinone-6′-carboxylic Acid: A Probe of the Minimum, Potent Pharmacophore of the Naturally Occurring Antitumor-Antibiotics. (1988) (0)
- Demonstration ofapronounced effect ofnoncovalent binding selectivity onthe(+)-CC-1065 DNA alkylation andidentification ofthepharmacophore ofthealkylation subunit (1991) (0)
- Synthesis of Vinblastine (2009) (0)
- Enantioselective Total Synthesis of (+)‐Duocarmycin A (+)‐(XI), epi‐(+) ‐Duocarmycin A (+)‐(XIII), and Their Unnatural Enantiomers. (1996) (0)
- Synthesis of Pyridazines by a Diels-Alder Strategy (2006) (0)
- Total Synthesis of the Teicoplanin Aglycon. (2000) (0)
- Total Synthesis of Combretastatin D-2: Intramolecular Ullmann Macrocyclization Reaction. (2010) (0)
- Diels-Alder Reactions of Heterocyclic Azadienes: Development of a Strategy for the Total Synthesis of Streptonigrin, Lavendamycin, and Synthetic Quinoline-5,8-quinones (1990) (0)
- Utilization of a Peptidomimetic Library to Bind and Sort a Retinal Vasculature–Targeting Subpopulation of Adult Bone Marrow–Derived Cells (2006) (0)
- Preparation and Inverse‐Electron‐Demand Diels–Alder Reaction of an Electron‐Deficient Diene: Methyl 2‐Oxo‐5,6,7,8‐Tetrahydro‐2H‐1‐Benzopyran‐3‐Carboxylate and 6‐Methoxy‐7‐Methoxycarbonyl‐1,2,3,4‐Tetrahydronaphthalane (2003) (0)
- Design and Total Synthesis of a Conformational Analog (I) of Bouvardin/ Deoxybouvardin. (1990) (0)
- A Concise Synthesis of the Fredericamycin A DEF Ring System: (4 + 2) Cycloaddition Reactions of 1‐Aza‐1,3‐butadienes. (1992) (0)
- , 466, H. Suschitzky, O. Meth-Cohn. The Royal Society of Chemistry, Burlington House, London WIV OBN, U.K. (1985), pp. 14 × 22 cm. ISBN: 0-442-30212-6. £95.00 ($138.00) (1986) (0)
- CCDC 253428: Experimental Crystal Structure Determination (2006) (0)
- Human GAR Tfase complex structure with polyglutamated 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid (2005) (0)
- Patent Number : ( 45 ) Date of Patent : 4 , 839 , 104 Jun . 13 , 1989 (2017) (0)
- Examination of the Role of the Duocarmycin SA Methoxy Substituents: Identification of the Minimum, Fully Potent DNA Binding Subunit. (1997) (0)
- A Novel Synthetic Route to Heterocyclic Quinones (2001) (0)
- ChemInform Abstract: Alternative Synthesis and Thermal Atropisomerism of a Fully Functionalized DEFG Ring System of Teicoplanin. (2002) (0)
- Preparation and Three‐Carbon + Two‐Carbon Cycloaddition of Cyclopropenone 1,3‐propanediol ketal: 5,5‐Dicyano‐4‐phenyl‐2‐cyclopenten‐1‐one 1,3‐propanediol ketal (2003) (0)
- Total Synthesis of (+)-CC-1065 and ent-(-)-CC-1065. (1988) (0)
- PREPARATION OF 3-METHYL-4-VINYL-1,2,5-OXADIAZOLE AND 3-METHYL-4-VINYL-1,2,5-THIADIAZOLE (1982) (0)
- Crystal Structure Analysis of a Phenhexyl/Oxazole/Carboxypyridine alpha-Ketoheterocycle Inhibitor Bound to a Humanized Variant of Fatty Acid Amide Hydrolase' (2009) (0)
- Tandem Free‐Radical Ring Expansion and 5‐exo‐dig 5‐Hexynyl Radical Cyclization: A Useful Approach to Fused Bicyclic Carbocycles. (1991) (0)
- Preparation of the 14-Membered L,L-Cycloisodityrosine Subunit of RP 66453. (2002) (0)
- Erratum: Total synthesis of natural (-)- and ent-(+)-4-desacetoxy-6,7- dihydrovindorosine and natural and ent-minovine: Oxadiazole tandem intramolecular diels-alder/1,3-dipolar cycloaddition reaction (Organic Letters (2005) 7 (741)) (2005) (0)
- Diels-Alder Reactions of Heterocyclic Azadienes: Total Synthesis of PDE I (XVIIIa), PDE II (XVIIIb), and PDE I Dimer Methyl Ester (XX). (1987) (0)
- Cycloadditions of Noncomplementary Substituted 1,2,3‐Triazines. (2015) (0)
- Primary amides of fatty acids for use in the sleeping introduction (1995) (0)
- Inhibition of Oleamide Hydrolase Catalyzed Hydrolysis of the Endogenous Sleep-Inducing Lipid cis-9-Octadecenamide. (1996) (0)
- Solution‐Phase Synthesis of Combinatorial Libraries Designed to Modulate Protein—Protein or Protein—DNA Interactions (2003) (0)
- Synthesis of Piericidins A1 and B1 (2006) (0)
- Synthesis, structure-activity relationship studies and evaluation of a TLR 3/8/9 agonist and its analogues (2021) (0)
- Improved preparative enzymatic glycosylation of vancomycin aglycon and analogues. (2022) (0)
- Oxidative Coupling of Methyl 6-Hydroxyindole-2-carboxylate with Primary Amines: Preparation of 2-Substituted Methyl Pyrrolo(2,3-e)benzoxazole-5-carboxylates. (1989) (0)
- Human Glycinamide Ribonucleotide Transformylase domain at pH 8.5 (2002) (0)
- Total Synthesis of (.+-.)-N2-(Phenylsulfonyl)-CPI, (.+-.)-CC-1065, (+)-CC-1065, ent-(-)-CC-1065, and the Precise, Functional Agents (.+-.)-CPI-CDPI2, (+)-CPI-CDPI2, and (-)-CPI-CDPI2 ((.+-.)-(3bR*,4aS*)-, (+)-(3bR,4aS)-, and (-)-(3bS, (1988) (0)
- Template for the synthesis of combinatorial libraries in solution (1996) (0)
- Indole N-Carbonyl Compounds: Preparation and Coupling of Indole-1-carboxylic Acid Anhydride. (1988) (0)
- Aryl Annulation: A Powerful Simplifying Retrosynthetic Disconnection (2022) (0)
- Synthesis of (+)-Fendleridine and (+)-1-Acetylaspidoalbidine (2010) (0)
- A Novel Class of CC-1065 and Duocarmycin Analogues Subject to Mitomycin-Related Reductive Activation (2000) (0)
- Studies on the Total Synthesis of Fredericamycin A (I): Development of an Intermolecular Alkyne-Chromium Carbene Complex Cyclization Approach to the ABCDE Ring System. (1989) (0)
- Cancer Therapeutics: Experimental and Clinical Agents, B.A. Teicher (Ed.). Humana Press (1997), xii + 451, ISBN: 0 896 03460 7 (1997) (0)
- Structural characterization of TLRs with novel agonists (2017) (0)
- Synthesis of Cytostatin (2007) (0)
- Polystyrene‐1‐ethyl‐3‐(3′‐dimethylaminopropyl)carbodiimide Hydrochloride (2003) (0)
- Total synthesis of the ramoplanin A2 and ramoplanose aglycon. (2002) (0)
- Human GAR Tfase complex structure with 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid (2005) (0)
- 3D-crystal structure of humanized-rat fatty acid amide hydrolase (FAAH) conjugated with 7-phenyl-1-(4-(pyridin-2-yl)oxazol-2-yl)heptan- 1-one, an alpha-ketooxazole (2009) (0)
- INVERSE ELECTRON DEMAND DIELS-ALDER REACTIONS OF 3-CARBOMETHOXY-2-PYRONES. CONTROLLED INTRODUCTION OF OXYGENATED AROMATICS: BENZENE, PHENOL, CATECHOL, RESORCINOL, AND PYROGALLOL ANNULATION. REGIOSPECIFIC TOTAL SYNTHESIS OF SENDAVERINE (1985) (0)
- (E,E)‐N‐Phenylsulfonyl‐4‐phenyl‐1‐aza‐1,3‐butadiene (2001) (0)
- Identification of novel and potent synthetic TLR agonists (2017) (0)
- Resolution of a CPzI Precursor, Synthesis and Biological Evaluation of (+) and (‐)‐N‐Boc‐CPzI: A Further Validation of the Relationship Between Chemical Solvolytic Stability and Cytotoxicity. (2000) (0)
- Crystal Structure Analysis of a Oleyl/Oxadiazole/pyridine Inhibitor Bound to a Humanized Variant of Fatty Acid Amide Hydrolase (2009) (0)
- CCDC 295588: Experimental Crystal Structure Determination (2006) (0)
- The structure of human glycinamide ribonucleotide transformylase in complex with 10R-methylthio-DDATHF. (2013) (0)
- Azadiene Diels-Alder Reactions: Scope and Applications (2003) (0)
- Total Synthesis of (‐)‐ and ent‐(+)‐4‐Desacetoxy‐5‐desethylvindoline. (2007) (0)
- Effective Thermal One-Carbon + Two-Carbon Cycloaddition to Cyclopropenone Ketals with Electron-Deficient Olefins: Cyclopropane Formation. Thermal Three-Carbon + Two-Atom Cycloaddition of Cyclopropenone Ketals with Carbon-Heteroatom Do (1985) (0)
- Diels-Alder Reactions of Heterocyclic Azadienes: Total Synthesis of PDE-II Methyl Ester. (1987) (0)
- A Modified Friedlaender Condensation for the Synthesis of 3- Hydroxyquinoline-2-carboxylates. (1996) (0)
- Total Synthesis of (+)- and ent-(-)-Duocarmycin SA (1995) (0)
- Synthesis of the Vancomycin CD and DE Ring Systems. (1997) (0)
- Synthesis of Phostriecin and Sultriecin (2010) (0)
- For the article ‘ ‘ A common variant in combination with a nonsense mutation in a member of the thioredoxin family causes primary ciliary dyskinesia (2007) (0)
- Synthesis of L,L-Isodityrosine (I). (1989) (0)
- Phenyl Selenoesters as Effective Precursors of Acyl Radicals for Use in Intermolecular Alkene Addition Reactions. (1989) (0)
- Towards rational drug design: crystal structures of glycinamide ribonucleotide transformylase (1996) (0)
- Synthesis of a Functionalized Rigid Bicyclo(2.2.1)heptane: A Useful Hapten for Eliciting Catalytic Antibodies. (1995) (0)
- Further Observations on the Lewis Acid-Catalyzed Benzylic Hydroperoxide Rearrangement: Use of a Boron Trifluoride/Hydrogen Peroxide, Preformed, Aged Reagent. (1987) (0)
- A Divergent de Novo Synthesis of Carbohydrates Based on an Accelerated Inverse Electron Demand Diels‐Alder Reaction of 1‐Oxa‐1,3‐butadienes. (1989) (0)
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