Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41 |
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Authors: | Jian Yang Long-Long Li Ju-Rong Li Jing-Xiang Yang Fang Zhang Gang Chen Rui Yu Wen-Jie Ouyang Shu-Wen Wu |
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Affiliation: | 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 |
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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. |
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Keywords: | Chiral gossypol derivative Amino acid derivative Oligopeptide derivative Taurine derivative Anti-HIV-1 Gp41 |
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