| Autor: |
Gregory Hollis, Tom Emm, Joseph Glenn, Kris Vaddi, Rajan Anand, Brian Metcalf, Douglas Keller, Peggy Scherle, Chen Lihua, Ke Zhang, Ganfeng Cao, Taisheng Huang, Sharon Diamond, Kim Solomon, Robert C. Newton, Chu-Biao Xue, Jiacheng Zhou, Meloni David, Steven Friedman, Nancy Contel, Anlai Wang, Changsheng Zheng, Bitao Zhao, Swamy Yeleswaram, Hao Feng, Ling Kong, Laurine G. Galya, Fredric Baribaud, Michael Xia, Niu Shin, Mei Li |
| Jazyk: |
angličtina |
| Rok vydání: |
2010 |
| Předmět: |
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| Popis: |
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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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