Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity

[Image: see text] 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...

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主要な著者: 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
フォーマット: Artigo
言語:Inglês
出版事項: American Chemical Society 2010
オンライン･アクセス:https://ncbi.nlm.nih.gov/pmc/articles/PMC4007949/
https://ncbi.nlm.nih.gov/pubmed/24900235
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml1001536
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