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Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41
Authors:Jian Yang  Long-Long Li  Ju-Rong Li  Jing-Xiang Yang  Fang Zhang  Gang Chen  Rui Yu  Wen-Jie Ouyang  Shu-Wen Wu
Institution:1. Department of Pharmacy, Renmin Hospital of Wuhan University, Wuhan 430060, China;2. The College of Life Sciences, State Key Laboratory of Virology, Modern Virology Research Center, Wuhan University, Wuhan 430072, China;3. Wuhan University School of Pharmaceutical Sciences, Wuhan 430071, China
Abstract:A series of novel or known water-soluble derivatives of chiral gossypol were synthesized and screened in vitro for their anti-HIV-1 activity. (?)-gossypol derivative was more active against HIV-1 than the corresponding (+)-gossypol derivative, respectively. Among these derivatives, d-glucosamine derivative of (?)-gossypol, oligopeptide derivative of (?)-gossypol and taurine derivative of (?)-gossypol, such as compounds 1a, 3a and 14a, showed significant inhibitory activities against HIV-1 replication, HIV-1 mediated cell-cell fusion and HIV gp41 6-helix bundle formation as some amino acid derivatives of (?)-gossypol.
Keywords:Chiral gossypol derivative  Amino acid derivative  Oligopeptide derivative  Taurine derivative  Anti-HIV-1  Gp41
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