Your browser doesn't support javascript.
loading
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.
Lai, Kwong Wah; Romero, F Anthony; Tsui, Vickie; Beresini, Maureen H; de Leon Boenig, Gladys; Bronner, Sarah M; Chen, Kevin; Chen, Zhongguo; Choo, Edna F; Crawford, Terry D; Cyr, Patrick; Kaufman, Susan; Li, Yingjie; Liao, Jiangpeng; Liu, Wenfeng; Ly, Justin; Murray, Jeremy; Shen, Weichao; Wai, John; Wang, Fei; Zhu, Caicai; Zhu, Xiaoyu; Magnuson, Steven.
Afiliação
  • Lai KW; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
  • Romero FA; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Tsui V; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States. Electronic address: vickie.tsui@aya.yale.edu.
  • Beresini MH; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • de Leon Boenig G; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Bronner SM; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Chen K; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
  • Chen Z; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
  • Choo EF; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Crawford TD; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Cyr P; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Kaufman S; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Li Y; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
  • Liao J; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
  • Liu W; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
  • Ly J; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Murray J; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Shen W; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
  • Wai J; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
  • Wang F; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
  • Zhu C; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
  • Zhu X; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
  • Magnuson S; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States. Electronic address: magnuson.steven@gene.com.
Bioorg Med Chem Lett ; 28(1): 15-23, 2018 01 01.
Article em En | MEDLINE | ID: mdl-29169673
ABSTRACT
A novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP, compound 35 (GNE-207), has been identified through SAR investigations focused on optimizing al bicyclic heteroarene to replace the aniline present in the published GNE-272 series. Compound 35 has excellent CBP potency (CBP IC50 = 1 nM, MYC EC50 = 18 nM), a selectively index of >2500-fold against BRD4(1), and exhibits a good pharmacokinetic profile.
Assuntos
Palavras-chave
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos de Bifenilo / Desenho de Fármacos / Fatores de Transcrição de p300-CBP Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2018 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos de Bifenilo / Desenho de Fármacos / Fatores de Transcrição de p300-CBP Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2018 Tipo de documento: Article