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The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).
Heffron, Timothy P; Heald, Robert A; Ndubaku, Chudi; Wei, BinQing; Augistin, Martin; Do, Steven; Edgar, Kyle; Eigenbrot, Charles; Friedman, Lori; Gancia, Emanuela; Jackson, Philip S; Jones, Graham; Kolesnikov, Aleksander; Lee, Leslie B; Lesnick, John D; Lewis, Cristina; McLean, Neville; Mörtl, Mario; Nonomiya, Jim; Pang, Jodie; Price, Steve; Prior, Wei Wei; Salphati, Laurent; Sideris, Steve; Staben, Steven T; Steinbacher, Stefan; Tsui, Vickie; Wallin, Jeffrey; Sampath, Deepak; Olivero, Alan G.
Afiliação
  • Heffron TP; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Heald RA; Argenta , Early Discovery Charles River, 7-9 Spire Green Centre, Flex Meadow, Harlow, EssexCM19 5TR, United Kingdom.
  • Ndubaku C; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Wei B; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Augistin M; Proteros Biostructures GmbH , Bunsenstr. 7aD, 82152 Martinsried, Germany.
  • Do S; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Edgar K; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Eigenbrot C; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Friedman L; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Gancia E; Argenta , Early Discovery Charles River, 7-9 Spire Green Centre, Flex Meadow, Harlow, EssexCM19 5TR, United Kingdom.
  • Jackson PS; Argenta , Early Discovery Charles River, 7-9 Spire Green Centre, Flex Meadow, Harlow, EssexCM19 5TR, United Kingdom.
  • Jones G; Argenta , Early Discovery Charles River, 7-9 Spire Green Centre, Flex Meadow, Harlow, EssexCM19 5TR, United Kingdom.
  • Kolesnikov A; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Lee LB; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Lesnick JD; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Lewis C; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • McLean N; Argenta , Early Discovery Charles River, 7-9 Spire Green Centre, Flex Meadow, Harlow, EssexCM19 5TR, United Kingdom.
  • Mörtl M; Proteros Biostructures GmbH , Bunsenstr. 7aD, 82152 Martinsried, Germany.
  • Nonomiya J; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Pang J; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Price S; Argenta , Early Discovery Charles River, 7-9 Spire Green Centre, Flex Meadow, Harlow, EssexCM19 5TR, United Kingdom.
  • Prior WW; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Salphati L; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Sideris S; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Staben ST; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Steinbacher S; Proteros Biostructures GmbH , Bunsenstr. 7aD, 82152 Martinsried, Germany.
  • Tsui V; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Wallin J; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Sampath D; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
  • Olivero AG; Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
J Med Chem ; 59(3): 985-1002, 2016 Feb 11.
Article em En | MEDLINE | ID: mdl-26741947
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Oxazepinas / Benzoxepinas / Desenho de Fármacos / Inibidores de Proteínas Quinases / Inibidores de Fosfoinositídeo-3 Quinase / Imidazóis / Antineoplásicos Tipo de estudo: Diagnostic_studies Limite: Animals / Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Oxazepinas / Benzoxepinas / Desenho de Fármacos / Inibidores de Proteínas Quinases / Inibidores de Fosfoinositídeo-3 Quinase / Imidazóis / Antineoplásicos Tipo de estudo: Diagnostic_studies Limite: Animals / Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Estados Unidos