Discovery of Potent and Selective RSK Inhibitors as Biological Probes

Rama Jain, Michelle Mathur, Jiong Lan, +13

Journal of Medicinal Chemistry

Drug TargetChemoprevention StrategyRsk Kinase FamilyChemical BiologyTumor Biology +15

Identification of a novel class of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents with protein tyrosine phosphatase inhibitory activity

Kevin R. Guertin, L Setti, Lida Qi, +14

Bioorganic & Medicinal Chemistry Letters

BiochemistryMedicineNatural SciencesMechanism Of ActionPharmacological Agent +7

Design and Discovery of <i>N</i>-(2-Methyl-5′-morpholino-6′-((tetrahydro-2<i>H</i>-pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers

Gisele Nishiguchi, Alice Rico, Huw R. Tanner, +39

Journal of Medicinal Chemistry

Drug TargetKras Mutant TumorsKinase InhibitorsChemical BiologyPharmaceutical Chemistry +15

Design and Discovery of <i>N</i>-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic

Savithri Ramurthy, Benjamin R. Taft, Robert J. Aversa, +45

Journal of Medicinal Chemistry

Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors

Paul A. Barsanti, Yue Pan, Yipin Lu, +18

ACS Medicinal Chemistry Letters

Pharmaceutical ScienceDrug TargetIndole MoietyPharmacotherapyCompound 13 +17

2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors

Abran Costales, Michelle Mathur, Savithri Ramurthy, +15

Bioorganic & Medicinal Chemistry Letters

2-Amino-7-substituted Benzoxazole AnalogsMedicinal ChemistryMedicinePharmacological AgentPharmacotherapy +3

Scaffold hopping towards potent and selective JAK3 inhibitors: Discovery of novel C-5 substituted pyrrolopyrazines

Javier de Vicente, Rémy C. Lemoine, Mark J. Bartlett, +16

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryBiochemistrySelective Jak3 InhibitorsNatural Sciences +7

Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles

Rémy C. Lemoine, Ann Petersen, L Setti, +7

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicineMembrane TransportPeptoidSecondary Amide Replacements +4

Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc

Rémy C. Lemoine, Ann Petersen, L Setti, +7

Bioorganic & Medicinal Chemistry Letters

Ccr5 Antagonist MaravirocMedicinal ChemistryHeterocyclicBiochemistryMedicine +7

Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists

Rémy C. Lemoine, Ann Petersen, L Setti, +7

Bioorganic & Medicinal Chemistry Letters

4-Aminopiperidine ReplacementBiochemistryFunctional SelectivityPharmacologyPharmacotherapy +5