Discovery and in vivo evaluation of (S)-N-(1-(7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease

Journal of Medicinal Chemistry

Volumn 58, Issue 1, 2015, Pages 480-511

  Cushing, Timothy D ^a   Hao, Xiaolin ^a   Shin, Youngsook ^a   Andrews, Kristin ^a   Brown, Matthew ^a   Cardozo, Mario ^a   Chen, Yi ^a   Duquette, Jason ^a   Fisher, Ben ^a   Gonzalez Lopez De Turiso, Felix ^a   He, Xiao ^a   Henne, Kirk R ^a   Hu, Yi Ling ^a   Hungate, Randall ^a   Johnson, Michael G ^a   Kelly, Ron C ^a   Lucas, Brian ^a   McCarter, John D ^a   McGee, Lawrence R ^a   Medina, Julio C ^a   San Miguel, Tisha ^a   Mohn, Deanna ^a   Pattaropong, Vatee ^a   Pettus, Liping H ^a   Reichelt, Andreas ^a   Rzasa, Robert M ^a   Seganish, Jennifer ^a   Tasker, Andrew S ^a   Wahl, Robert C ^a   Wannberg, Sharon ^a   Whittington, Douglas A ^a   Whoriskey, John ^a   Yu, Gang ^a   Zalameda, Leeanne ^a   Zhang, Dawei ^a   Metz, Daniela P ^a   more..

^a AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

(2 CHLORO 8 METHYLQUINOLIN 3 YL)METHANOL; (8 METHYL 2 2 TOLYLQUINOLIN 3 YL)METHANOL; 1 (2 CHLORO 5,7 DIFLUOROQUINOLIN 3 YL)ETHANOL; 1 (2 CHLORO 7 FLUOROQUINOLIN 3 YL)ETHANOL; 1 [8 CHLORO 2 (2 CHLOROPHENYL)QUINOLIN 3 YL]ETHANOL; 1 [8 CHLORO 2 (2 METHYLPYRIDIN 3 YL)QUINOLIN 3 YL]ETHANOL; 1 [8 METHYL 2 (2 TOLYL)QUINOLIN 3 YL]ETHANOL; 2 (2 METHOXYPHENYL) 8 METHYLQUINOLINE 3 CARBALDEHYDE; 3 ETHYNYL 8 METHYL 2 (2 TOLYL)QUINOLINE; 3 [(7H PURIN 6 YL)ETHYNYL] 8 METHYL 2 (2 TOLYL)QUINOLINE; 3 [(9H PURIN 6 YLOXY)METHYL] 2 (2 METHOXYPHENYL) 8 METHYLQUINOLINE; 3 [(9H PURIN 6 YLTHIO)METHYL] 2 (2 METHOXYPHENYL) 8 METHYLQUINOLINE; 3 [1 [(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)OXY]ETHYL] 8 METHYL 2 (2 TOLYL)QUINOLINE; 3 [2 (7H PURIN 6 YL)ETHYL] 8 METHYL 2 (2 TOLYL)QUINOLINE; 3 [[(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)OXY]METHYL] 8 METHYL 2 (2 TOLYL)QUINOLINE; 3 [[(9H PURIN 6 YL)OXY]METHYL] 8 METHYL 2 (2 TOLYL)QUINOLINE; 4 [1 (6 CHLORO 3 METHYLCINNOLIN 4 YL] 3,3 DIMETHYLINDOLIN 6 YL)MORPHOLINE; 8 CHLORO 2 (2 CHLOROPHENYL)QUINOLINE 3 CARBALDEHYDE; 8 CHLORO 2 (2 METHYLPYRIDIN 3 YL)QUINOLINE 3 CARBALDEHYDE; 8 CHLORO 2 (3 FLUOROPHENYL)QUINOLINE 3 CARBALDEHYDE; 8 METHYL 2 (2 METHYLPHENYL)QUINOLINE 3 CARBALDEHYDE; ANTIINFLAMMATORY AGENT; IMMUNOMODULATING AGENT; N [(8 METHYL 2 2 TOLYLQUINOLIN 3 YL)METHYL] 9H PURIN 6 AMINE; N [1 [7 FLUORO 2 (PYRIDIN 2 YL)QUINOLIN 3 YL]ETHYL] 9H PURIN 6 AMINE; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; QUINOLINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; [2 (2 METHOXYPHENYL) 8 METHYLQUINOLIN 3 YL]METHANOL; [8 CHLORO 2 (3 FLUOROPHENYL)QUINOLIN 3 YL]METHANOL; ADENOSINE; N-(1-(7-FLUORO-2-(PYRIDIN-2-YL)QUINOLIN-3-YL)ETHYL)-9H-PURIN-6-AMINE; PHOSPHATIDYLINOSITOL 4,5 BISPHOSPHATE 3 KINASE; PIK3CD PROTEIN, HUMAN; PROTEIN BINDING; PROTEIN KINASE INHIBITOR;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; AUTOIMMUNE DISEASE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG SCREENING; DRUG SOLUBILITY; DRUG SYNTHESIS; ENZYME PHOSPHORYLATION; FEMALE; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; IN VIVO STUDY; INFLAMMATION; INTRINSIC CLEARANCE; LIVER CLEARANCE; METABOLIC CLEARANCE; NONHUMAN; PHYSICAL CHEMISTRY; RAT; STRUCTURE ACTIVITY RELATION; ANIMAL; ANTAGONISTS AND INHIBITORS; AUTOIMMUNE DISEASES; BAGG ALBINO MOUSE; CELL CULTURE; CHEMICAL MODEL; CHEMICAL STRUCTURE; CHEMISTRY; DISEASE MODEL; DRUG DEVELOPMENT; LEWIS RAT; METABOLISM; PROTEIN TERTIARY STRUCTURE; SF9 CELL LINE; TRANSGENIC MOUSE; X RAY CRYSTALLOGRAPHY;

ADENOSINE; ANIMALS; AUTOIMMUNE DISEASES; CELLS, CULTURED; CLASS I PHOSPHATIDYLINOSITOL 3-KINASES; CRYSTALLOGRAPHY, X-RAY; DISEASE MODELS, ANIMAL; DRUG DISCOVERY; FEMALE; HUMANS; INFLAMMATION; MICE, INBRED BALB C; MICE, TRANSGENIC; MODELS, CHEMICAL; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; QUINOLINES; RATS, INBRED LEW; SF9 CELLS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84925814143     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501624r     Document Type: Article

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