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Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.
Bryan, Marian C; Burdick, Daniel J; Chan, Bryan K; Chen, Yuan; Clausen, Saundra; Dotson, Jennafer; Eigenbrot, Charles; Elliott, Richard; Hanan, Emily J; Heald, Robert; Jackson, Philip; La, Hank; Lainchbury, Michael; Malek, Shiva; Mann, Sam E; Purkey, Hans E; Schaefer, Gabriele; Schmidt, Stephen; Seward, Eileen; Sideris, Steve; Wang, Shumei; Yen, Ivana; Yu, Christine; Heffron, Timothy P.
Afiliação
  • Bryan MC; Genentech , South San Francisco, California 94080, United States.
  • Burdick DJ; Genentech , South San Francisco, California 94080, United States.
  • Chan BK; Genentech , South San Francisco, California 94080, United States.
  • Chen Y; Genentech , South San Francisco, California 94080, United States.
  • Clausen S; Genentech , South San Francisco, California 94080, United States.
  • Dotson J; Genentech , South San Francisco, California 94080, United States.
  • Eigenbrot C; Genentech , South San Francisco, California 94080, United States.
  • Elliott R; Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Hanan EJ; Genentech , South San Francisco, California 94080, United States.
  • Heald R; Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Jackson P; Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • La H; Genentech , South San Francisco, California 94080, United States.
  • Lainchbury M; Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Malek S; Genentech , South San Francisco, California 94080, United States.
  • Mann SE; Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Purkey HE; Genentech , South San Francisco, California 94080, United States.
  • Schaefer G; Genentech , South San Francisco, California 94080, United States.
  • Schmidt S; Genentech , South San Francisco, California 94080, United States.
  • Seward E; Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Sideris S; Genentech , South San Francisco, California 94080, United States.
  • Wang S; Genentech , South San Francisco, California 94080, United States.
  • Yen I; Genentech , South San Francisco, California 94080, United States.
  • Yu C; Genentech , South San Francisco, California 94080, United States.
  • Heffron TP; Genentech , South San Francisco, California 94080, United States.
ACS Med Chem Lett ; 7(1): 100-4, 2016 Jan 14.
Article em En | MEDLINE | ID: mdl-26819674
The rapid advancement of a series of noncovalent inhibitors of T790M mutants of EGFR is discussed. The optimization of pyridone 1, a nonselective high-throughput screening hit, to potent molecules with high levels of selectivity over wtEGFR and the broader kinome is described herein.
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Estados Unidos