Structure-based design of thienobenzoxepin inhibitors of PI3-kinase

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 13, 2011, Pages 4054-4058

  Staben, Steven T ^a   Siu, Michael ^a   Goldsmith, Richard ^a   Olivero, Alan G ^a   Do, Steven ^a   Burdick, Daniel J ^a   Heffron, Timothy P ^a   Dotson, Jenna ^a   Sutherlin, Daniel P ^a   Zhu, Bing Yan ^a   Tsui, Vickie ^a   Le, Hoa ^a   Lee, Leslie ^a   Lesnick, John ^a   Lewis, Cristina ^a   Murray, Jeremy M ^a   Nonomiya, Jim ^a   Pang, Jodie ^a   Prior, Wei Wei ^a   Salphati, Laurent ^a   Rouge, Lionel ^a   Sampath, Deepak ^a   Sideris, Steve ^a   Wiesmann, Christian ^a   Wu, Ping ^a   more..

^a GENENTECH INC   (United States)

Author keywords

PI3 kinase; Structure based design

Indexed keywords

2 (1H INDAZOL 4 YL) 6 (4 METHANESULFONYL 1 PIPERAZINYLMETHYL) 4 MORPHOLINOTHIENO[3,2 D]PYRIMIDINE; BENZOXEPIN DERIVATIVE; GNE 614; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CELL STRAIN MCF 7; CONTROLLED STUDY; CRYSTALLIZATION; DRUG POTENTIATION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; METABOLISM; MOLECULAR MODEL; MOUSE; NONHUMAN; STRUCTURE ANALYSIS; TUMOR XENOGRAFT;

ANIMALS; BENZOXEPINS; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME ACTIVATION; ENZYME INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; MICE; MOLECULAR STRUCTURE; PHOSPHATIDYLINOSITOL 3-KINASES; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 79958698832     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.04.124     Document Type: Article

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