Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 9, 2013, Pages 2606-2613

  Staben, Steven T ^a   Ndubaku, Chudi ^a   Blaquiere, Nicole ^a   Belvin, Marcia ^a   Bull, Richard J ^b   Dudley, Danette ^a   Edgar, Kyle ^a   Gray, Daniel ^a   Heald, Robert ^b   Heffron, Timothy P ^a   Jones, Graham E ^b   Jones, Mark ^b   Kolesnikov, Aleks ^a   Lee, Leslie ^a   Lesnick, John ^a   Lewis, Cristina ^a   Murray, Jeremy ^a   McLean, Neville J ^b   Nonomiya, Jim ^a   Olivero, Alan G ^a   Ord, Rachel ^b   Pang, Jodie ^a   Price, Stephen ^b   Prior, Wei Wei ^a   Rouge, Lionel ^a   Salphati, Laurent ^a   Sampath, Deepak ^a   Wallin, Jeff ^a   Wang, Lan ^a   Wei, Binqing ^a   Weismann, Christian ^a   Wu, Ping ^a   more..

^a GENENTECH INC   (United States)

^b Early Discovery Charles River   (United Kingdom)

Author keywords

Isoform selectivity; PI3 kinase; Structure based ligand design

Indexed keywords

BENZOXEPIN DERIVATIVE; HETEROCYCLIC COMPOUND; ISOENZYME; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHATIDYLINOSITOL 3 KINASE ALPHA; PHOSPHATIDYLINOSITOL 3 KINASE DELTA; PHOSPHATIDYLINOSITOL 3 KINASE GAMMA; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PICTILISIB; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CELL LINE; CELL PROLIFERATION; CONTROLLED STUDY; DOSE RESPONSE; DRUG SELECTIVITY; GENE SILENCING; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MOUSE; NONHUMAN; SINGLE DRUG DOSE;

BENZOXEPINS; BINDING SITES; CELL PROLIFERATION; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HUMANS; MCF-7 CELLS; MOLECULAR DOCKING SIMULATION; PHOSPHATIDYLINOSITOL 3-KINASE; PROTEIN ISOFORMS; PROTEIN STRUCTURE, TERTIARY; PROTO-ONCOGENE PROTEINS C-AKT; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES;

EID: 84876139290     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.02.102     Document Type: Article

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