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A Strategy to Minimize Reactive Metabolite Formation: Discovery of (S)-4-(1-Cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a Potent, Orally Bioavailable Corticotropin-Releasing Factor-1 Receptor Antagonist

Journal of medicinal chemistry, 2009-12, Vol.52 (23), p.7653-7668

2009

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Reductively activated disulfide prodrugs of paclitaxel

Bioorganic & medicinal chemistry letters, 2002-12, Vol.12 (24), p.3591-3594

2002

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Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF1) receptor antagonist BMS-665053 leading to improved oral bioavailability

Bioorganic & medicinal chemistry letters, 2017-03, Vol.27 (6), p.1360-1363

2017

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Serendipitous oxidation product of BIBN4096BS: A potent CGRP receptor antagonist

Bioorganic & medicinal chemistry letters, 2014-06, Vol.24 (12), p.2744-2748

2014

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Comparative biotransformation of pyrazinone-containing corticotropin-releasing factor receptor-1 antagonists: minimizing the reactive metabolite formation

Drug metabolism and disposition, 2010-01, Vol.38 (1), p.5-15

2010

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Chiral separation of potent corticotropin-releasing factor-1 receptor antagonists by supercritical fluid chromatography

Journal of pharmaceutical and biomedical analysis, 2011-02, Vol.54 (3), p.602-606

2011

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2-Aryl-2,2-difluoroacetamide FKBP12 Ligands: Synthesis and X-ray Structural Studies

Organic letters, 2001-12, Vol.3 (25), p.3987-3990

2001

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Separation of maxi-K channel opening 3-substitued-4-arylquinolinone atropisomers by enantioselective supercritical fluid chromatography

Journal of pharmaceutical and biomedical analysis, 2008-12, Vol.48 (4), p.1120-1126

2008

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Development and Activities of a New Melphalan Prodrug Designed for Tumor-Selective Activation

Bioconjugate chemistry, 1998-03, Vol.9 (2), p.255-259

1998

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Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists

Bioorganic & medicinal chemistry letters, 2010-06, Vol.20 (12), p.3669-3674

2010

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Design, synthesis and evaluation of constrained tetrahydroimidazopyrimidine derivatives as antagonists of corticotropin-releasing factor type 1 receptor (CRF 1R)

Bioorganic & medicinal chemistry letters, 2010-03, Vol.20 (6), p.1905-1909

2010

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Atropisomeric 3-(β-hydroxyethyl)-4-arylquinolin-2-ones as Maxi-K Potassium Channel Openers

Journal of medicinal chemistry, 2007-03, Vol.50 (5), p.1050-1057

2007

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Cephalosporin prodrugs of paclitaxel for immunologically specific activation by L-49-sFv-β-Lactamase fusion protein

Bioorganic & medicinal chemistry letters, 2003-02, Vol.13 (3), p.539-542

2003

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Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes

Bioorganic & medicinal chemistry letters, 2005-10, Vol.15 (19), p.4286-4290

2005

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Cephalosporin Derivatives of Doxorubicin as Prodrugs for Activation by Monoclonal Antibody-.beta.-Lactamase Conjugates

Journal of medicinal chemistry, 1995-04, Vol.38 (8), p.1380-1385

1995

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Comparison of Recombinant and Synthetically Formed Monoclonal Antibody-β-Lactamase Conjugates for Anticancer Prodrug Activation

Bioconjugate chemistry, 1999-11, Vol.10 (6), p.1084-1089

1999

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Immunologically Specific Activation of a Cephalosporin Derivative of Mitomycin C by Monoclonal Antibody β-Lactamase Conjugates

Journal of medicinal chemistry, 1997-08, Vol.40 (17), p.2788-2792

1997

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Generation of cytotoxic agents by targeted enzymes

Bioconjugate chemistry, 1993-01, Vol.4 (1), p.3-9

1993

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Prodrugs of doxorubicin and melphalan and their activation by a monoclonal antibody-penicillin-G amidase conjugate

Journal of medicinal chemistry, 1993-04, Vol.36 (7), p.919-923

1993

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Monoclonal antibody-.beta.-lactamase conjugates for the activation of a cephalosporin mustard prodrug

Bioconjugate chemistry, 1992-03, Vol.3 (2), p.176-181

1992

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Antitumor activities of a cephalosporin prodrug in combination with monoclonal antibody-.beta.-lactamase conjugates

Bioconjugate chemistry, 1993-09, Vol.4 (5), p.334-340

1993

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Poly(ethylene glycol)-Doxorubicin Conjugates Containing .beta.-Lactamase-Sensitive Linkers

Bioconjugate chemistry, 1995-07, Vol.6 (4), p.389-394

1995

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Synthesis and binding studies of crown ethers bearing pharmacophoric groups: epoxy lariat crown ethers

Journal of organic chemistry, 1984-06, Vol.49 (13), p.2423-2427

1984

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A Strategy to Minimize Reactive Metabolite Formation: Discovery of (S)-4-(1-Cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a Potent, Orally Bioavailable Corticotropin-Releasing Factor-1 Receptor Antagonist

Reductively activated disulfide prodrugs of paclitaxel

Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF1) receptor antagonist BMS-665053 leading to improved oral bioavailability

Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor

Serendipitous oxidation product of BIBN4096BS: A potent CGRP receptor antagonist

Comparative biotransformation of pyrazinone-containing corticotropin-releasing factor receptor-1 antagonists: minimizing the reactive metabolite formation

Chiral separation of potent corticotropin-releasing factor-1 receptor antagonists by supercritical fluid chromatography

2-Aryl-2,2-difluoroacetamide FKBP12 Ligands: Synthesis and X-ray Structural Studies

Separation of maxi-K channel opening 3-substitued-4-arylquinolinone atropisomers by enantioselective supercritical fluid chromatography

Development and Activities of a New Melphalan Prodrug Designed for Tumor-Selective Activation

Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists

Design, synthesis and evaluation of constrained tetrahydroimidazopyrimidine derivatives as antagonists of corticotropin-releasing factor type 1 receptor (CRF 1R)

Atropisomeric 3-(β-hydroxyethyl)-4-arylquinolin-2-ones as Maxi-K Potassium Channel Openers

Cephalosporin prodrugs of paclitaxel for immunologically specific activation by L-49-sFv-β-Lactamase fusion protein

Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes

Cephalosporin Derivatives of Doxorubicin as Prodrugs for Activation by Monoclonal Antibody-.beta.-Lactamase Conjugates

Comparison of Recombinant and Synthetically Formed Monoclonal Antibody-β-Lactamase Conjugates for Anticancer Prodrug Activation

Immunologically Specific Activation of a Cephalosporin Derivative of Mitomycin C by Monoclonal Antibody β-Lactamase Conjugates

Generation of cytotoxic agents by targeted enzymes

Prodrugs of doxorubicin and melphalan and their activation by a monoclonal antibody-penicillin-G amidase conjugate

Monoclonal antibody-.beta.-lactamase conjugates for the activation of a cephalosporin mustard prodrug

Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2‑f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor

Antitumor activities of a cephalosporin prodrug in combination with monoclonal antibody-.beta.-lactamase conjugates

Poly(ethylene glycol)-Doxorubicin Conjugates Containing .beta.-Lactamase-Sensitive Linkers

Synthesis and binding studies of crown ethers bearing pharmacophoric groups: epoxy lariat crown ethers

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