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Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.
Xue, Chu-Biao; Chen, Lihua; Cao, Ganfeng; Zhang, Ke; Wang, Anlai; Meloni, David; Glenn, Joseph; Anand, Rajan; Xia, Michael; Kong, Ling; Huang, Taisheng; Feng, Hao; Zheng, Changsheng; Li, Mei; Galya, Laurine; Zhou, Jiacheng; Shin, Niu; Baribaud, Fredric; Solomon, Kim; Scherle, Peggy; Zhao, Bitao; Diamond, Sharon; Emm, Tom; Keller, Douglas; Contel, Nancy; Yeleswaram, Swamy; Vaddi, Kris; Hollis, Gregory; Newton, Robert; Friedman, Steven; Metcalf, Brian.
Afiliação
  • Xue CB; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Chen L; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Cao G; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Zhang K; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Wang A; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Meloni D; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Glenn J; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Anand R; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Xia M; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Kong L; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Huang T; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Feng H; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Zheng C; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Li M; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Galya L; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Zhou J; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Shin N; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Baribaud F; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Solomon K; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Scherle P; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Zhao B; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Diamond S; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Emm T; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Keller D; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Contel N; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Yeleswaram S; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Vaddi K; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Hollis G; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Newton R; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Friedman S; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
  • Metcalf B; Incyte Corporation, Experimental Station E336, Wilmington, Delaware 19880.
ACS Med Chem Lett ; 1(9): 483-7, 2010 Dec 09.
Article em En | MEDLINE | ID: mdl-24900235
ABSTRACT
To identify a CCR5 antagonist as an HIV-1 entry inhibitor, we designed a novel series of indane derivatives based on conformational considerations. Modification on the indane ring led to the discovery of compound 22a (INCB9471) that exhibited high affinity for CCR5, potent anti-HIV-1 activity, high receptor selectivity, excellent oral bioavailability, and a tolerated safety profile. INCB9471 has entered human clinical trials.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2010 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2010 Tipo de documento: Article