Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: Synthesis, SAR, and in vivo anti-inflammatory activity

Journal of Medicinal Chemistry

Volumn 49, Issue 19, 2006, Pages 5671-5686

  DiMauro, Erin F ^a   Newcomb, John ^a   Nunes, Joseph J ^a   Bemis, Jean E ^a   Boucher, Christina ^a   Buchanan, John L ^a   Buckner, William H ^a   Cee, Victor J ^a   Chai, Lilly ^a   Deak, Holly L ^a   Epstein, Linda F ^a   Faust, Ted ^a   Gallant, Paul ^a   Geuns Meyer, Stephanie D ^a   Gore, Anu ^b   Gu, Yan ^a   Henkle, Brad ^b   Hodous, Brian L ^a   Hsieh, Faye ^b   Huang, Xin ^a   Kim, Joseph L ^a   Lee, Josie H ^a   Martin, Matthew W ^a   Masse, Craig E ^a   McGowan, David C ^a   Metz, Daniela ^b   Mohn, Deanna ^b   Morgenstern, Kurt A ^a   Oliveira Dos Santos, Antonio ^a   Patel, Vinod F ^a   Powers, David ^a   Rose, Paul E ^a   Schneider, Stephen ^a   Tomlinson, Susan A ^a   Tudor, Yan Yan ^a   Turci, Susan M ^a   Welcher, Andrew A ^b   White, Ryan D ^a   Zhao, Huilin ^a   Zhu, Li ^b   Zhu, Xiaotian ^a   more..

^a Building 1000 ^*  (United States)

^b AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 METHYL 3 [2 (2 MORPHOLINOETHYLAMINO)QUINAZOLIN 6 YL] N [3 (TRIFLUOROMETHYL)PHENYL]BENZAMIDE; 4 METHYL 3 [2 (METHYLAMINO)QUINAZOLIN 6 YL] N [2 (1 METHYLPIPERIDIN 4 YLOXY) 5 (TRIFLUOROMETHYL)PHENYL]BENZAMIDE; ANTIINFLAMMATORY AGENT; CD3 ANTIBODY; INTERLEUKIN 2; PROTEIN KINASE LCK; QUINAZOLINE DERIVATIVE; T LYMPHOCYTE RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; ARTICLE; CELL MATURATION; CONTROLLED STUDY; CYTOKINE PRODUCTION; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME INHIBITOR INTERACTION; FEMALE; HUMAN; HUMAN CELL; LYMPHOCYTE PROLIFERATION; MALE; MOUSE; NONHUMAN; RAT; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; T LYMPHOCYTE ACTIVATION;

ADMINISTRATION, ORAL; ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; BENZAMIDES; BIOLOGICAL AVAILABILITY; CELL PROLIFERATION; CELLS, CULTURED; FEMALE; HUMANS; INTERLEUKIN-2; LYMPHOCYTE SPECIFIC PROTEIN TYROSINE KINASE P56(LCK); MALE; MICE; MICE, INBRED BALB C; MODELS, MOLECULAR; QUINAZOLINES; RATS; RATS, SPRAGUE-DAWLEY; STRUCTURE-ACTIVITY RELATIONSHIP; T-LYMPHOCYTES; TUMOR NECROSIS FACTOR-ALPHA;

EID: 33748851665     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0605482     Document Type: Article

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