کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1254715 | 971387 | 2014 | 5 صفحه PDF | دانلود رایگان |

A series of novel gossypol derivatives were synthesized and screened for their in vitro anti-HIV-1 activity. The results showed that replacing the aldehyde groups of gossypol with certain oligopeptides and d-glucosamine not only reduced the cytotoxicity of gossypol derivatives but also enhanced their antiviral activity against HIV-1. Interestingly, d-glucosamine derivative of gossypol that lacked the COONa group also exhibited the same potent anti-HIV-1 activity as oligopeptide derivatives with the COONa group. These compounds blocked the entry of HIV-1IIIB into target cell, which was similar to T20. Furthermore, the molecular docking analysis rationalized their anti-HIV-1 activity. The results also implied that certain oligopeptides and d-glucosamine were important moities to prepare gossypol derivatives as HIV-1 entry inhibitors besides certain amino acids.
Certain oligopeptides and d-glucosamine are important moities to prepare gossypol derivatives as HIV-1 entry inhibitors besides certain amino acids.Figure optionsDownload as PowerPoint slide
Journal: Chinese Chemical Letters - Volume 25, Issue 7, July 2014, Pages 1052–1056