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ACS Med Chem Lett
; 1(9): 483-7, 2010 Dec 09.
Article
in English
| 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.