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Cyclin-Dependent Kinase (CDK) Inhibitors: Structure–Activity Relationships and Insights into the CDK‑2 Selectivity of 6‑Substituted 2‑Arylaminopurines

Journal of medicinal chemistry, 2017-03, Vol.60 (5), p.1746-1767

2017

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(2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Journal of medicinal chemistry, 2005-01, Vol.48 (1), p.141-151

2005

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Hit-to-Lead Optimization and Discovery of 5‑((5-([1,1′-Biphenyl]-4-yl)-6-chloro‑1H‑benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase

Journal of medicinal chemistry, 2017-11, Vol.60 (21), p.9040-9052

2017

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Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3‑Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders

Journal of medicinal chemistry, 2017-06, Vol.60 (12), p.5193-5208

2017

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Novel Indole-Based Peroxisome Proliferator-Activated Receptor Agonists: Design, SAR, Structural Biology, and Biological Activities

Journal of medicinal chemistry, 2005-12, Vol.48 (26), p.8194-8208

2005

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Arylcyclopropanecarboxyl Guanidines as Novel, Potent, and Selective Inhibitors of the Sodium Hydrogen Exchanger Isoform-1

Journal of medicinal chemistry, 2001-09, Vol.44 (20), p.3302-3310

2001

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A Novel Series of Highly Potent Benzimidazole-Based Microsomal Triglyceride Transfer Protein Inhibitors

Journal of medicinal chemistry, 2001-03, Vol.44 (6), p.851-856

2001

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Dual Angiotensin II and Endothelin A Receptor Antagonists: Synthesis of 2‘-Substituted N-3-Isoxazolyl Biphenylsulfonamides with Improved Potency and Pharmacokinetics

Journal of medicinal chemistry, 2005-01, Vol.48 (1), p.171-179

2005

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Structure−Activity Relationship and Mechanism of Action Studies of Manzamine Analogues for the Control of Neuroinflammation and Cerebral Infections

Journal of medicinal chemistry, 2010-01, Vol.53 (1), p.61-76

2010

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Design, Synthesis, and Evaluation of 3,4-Dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as Inhibitors of Poly(ADP-Ribose) Polymerase

Journal of medicinal chemistry, 2004-10, Vol.47 (22), p.5467-5481

2004

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Hit-to-Lead Optimization and Discovery of 5-((5-([1,1′-Biphenyl]-4-yl)-6-chloro-1 H -benzo[ d ]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase

Journal of medicinal chemistry, 2017-11, Vol.60 (21), p.9040-9052

2017

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Orally Active Squalene Synthase Inhibitors: Bis((acyloxy)alkyl) Prodrugs of the α-Phosphonosulfonic Acid Moiety

Journal of medicinal chemistry, 1996-02, Vol.39 (3), p.661-664

1996

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Discovery of Potent and Selective Dipeptidyl Peptidase IV Inhibitors Derived from β-Aminoamides Bearing Subsituted Triazolopiperazines

Journal of medicinal chemistry, 2008-02, Vol.51 (3), p.589-602

2008

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Novel N-Arylpyrazolo[3,2-c]-Based Ligands for the Glucocorticoid Receptor: Receptor Binding and in Vivo Activity

Journal of medicinal chemistry, 2004-05, Vol.47 (10), p.2441-2452

2004

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Discovery of Highly Potent and Selective Pan-Aurora Kinase Inhibitors with Enhanced in Vivo Antitumor Therapeutic Index

Journal of medicinal chemistry, 2012-04, Vol.55 (7), p.3250-3260

2012

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Synthesis and Discovery of Macrocyclic Polyoxygenated Bis-7-azaindolylmaleimides as a Novel Series of Potent and Highly Selective Glycogen Synthase Kinase-3β Inhibitors

Journal of medicinal chemistry, 2003-09, Vol.46 (19), p.4021-4031

2003

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Studies on Quinazolines and 1,2,4-Benzothiadiazine 1,1-Dioxides. 8. , Synthesis and Pharmacological Evaluation of Tricyclic Fused Quinazolines and 1,2,4-Benzothiadiazine 1,1-Dioxides as Potential α1-Adrenoceptor Antagonists

Journal of medicinal chemistry, 1998-08, Vol.41 (17), p.3128-3141

1998

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Anti-AIDS Agents. 52. † Synthesis and Anti-HIV Activity of Hydroxymethyl (3‘R,4‘R)-3‘,4‘-Di-O-(S)-camphanoyl-(+)-cis-khellactone Derivatives

Journal of medicinal chemistry, 2004-01, Vol.47 (3), p.756-760

2004

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Discovery of a Potent, Nonpolyglutamatable Inhibitor of Glycinamide Ribonucleotide Transformylase

Journal of medicinal chemistry, 2006-05, Vol.49 (10), p.2998-3002

2006

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Discovery of Potent and Selective Dipeptidyl Peptidase IV Inhibitors Derived from [beta]-Aminoamides Bearing Subsituted Triazolopiperazines

Journal of medicinal chemistry, 2008-06, Vol.51 ((3) ; 2008)

2008

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S-(N-Aryl-N-hydroxycarbamoyl)glutathione Derivatives Are Tight-Binding Inhibitors of Glyoxalase I and Slow Substrates for Glyoxalase II

Journal of medicinal chemistry, 1994-07, Vol.37 (14), p.2161-2166

1994

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Cyclin-Dependent Kinase (CDK) Inhibitors: Structure–Activity Relationships and Insights into the CDK‑2 Selectivity of 6‑Substituted 2‑Arylaminopurines

(2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials

An Alkynylpyrimidine-Based Covalent Inhibitor That Targets a Unique Cysteine in NF-κB-Inducing Kinase

Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials

Hit-to-Lead Optimization and Discovery of 5‑((5-([1,1′-Biphenyl]-4-yl)-6-chloro‑1H‑benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3‑Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders

Novel Indole-Based Peroxisome Proliferator-Activated Receptor Agonists: Design, SAR, Structural Biology, and Biological Activities

Arylcyclopropanecarboxyl Guanidines as Novel, Potent, and Selective Inhibitors of the Sodium Hydrogen Exchanger Isoform-1

A Novel Series of Highly Potent Benzimidazole-Based Microsomal Triglyceride Transfer Protein Inhibitors

Dual Angiotensin II and Endothelin A Receptor Antagonists: Synthesis of 2‘-Substituted N-3-Isoxazolyl Biphenylsulfonamides with Improved Potency and Pharmacokinetics

Structure−Activity Relationship and Mechanism of Action Studies of Manzamine Analogues for the Control of Neuroinflammation and Cerebral Infections

Design, Synthesis, and Evaluation of 3,4-Dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as Inhibitors of Poly(ADP-Ribose) Polymerase

Hit-to-Lead Optimization and Discovery of 5-((5-([1,1′-Biphenyl]-4-yl)-6-chloro-1 H -benzo[ d ]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase

Orally Active Squalene Synthase Inhibitors: Bis((acyloxy)alkyl) Prodrugs of the α-Phosphonosulfonic Acid Moiety

Discovery of Potent and Selective Dipeptidyl Peptidase IV Inhibitors Derived from β-Aminoamides Bearing Subsituted Triazolopiperazines

Novel N-Arylpyrazolo[3,2-c]-Based Ligands for the Glucocorticoid Receptor: Receptor Binding and in Vivo Activity

Discovery of Highly Potent and Selective Pan-Aurora Kinase Inhibitors with Enhanced in Vivo Antitumor Therapeutic Index

Synthesis and Discovery of Macrocyclic Polyoxygenated Bis-7-azaindolylmaleimides as a Novel Series of Potent and Highly Selective Glycogen Synthase Kinase-3β Inhibitors

Studies on Quinazolines and 1,2,4-Benzothiadiazine 1,1-Dioxides. 8. , Synthesis and Pharmacological Evaluation of Tricyclic Fused Quinazolines and 1,2,4-Benzothiadiazine 1,1-Dioxides as Potential α1-Adrenoceptor Antagonists

Anti-AIDS Agents. 52. † Synthesis and Anti-HIV Activity of Hydroxymethyl (3‘R,4‘R)-3‘,4‘-Di-O-(S)-camphanoyl-(+)-cis-khellactone Derivatives

Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3,5-difluoro- 6-[3-(4,5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylglycine (ZK-807834): A Potent, Selective, and Orally Active Inhibitor of the Blood Coagulation Enzyme Factor Xa

Discovery of a Potent, Nonpolyglutamatable Inhibitor of Glycinamide Ribonucleotide Transformylase

Discovery of Potent and Selective Dipeptidyl Peptidase IV Inhibitors Derived from [beta]-Aminoamides Bearing Subsituted Triazolopiperazines

S-(N-Aryl-N-hydroxycarbamoyl)glutathione Derivatives Are Tight-Binding Inhibitors of Glyoxalase I and Slow Substrates for Glyoxalase II

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