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ID: ALA4177704

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41.

Authors: Yang J, Li LL, Li JR, Yang JX, Zhang F, Chen G, Yu R, Ouyang WJ, Wu SW.

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.

CiteXplore: 29162455

DOI: 10.1016/j.bmcl.2017.08.049