کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1254715 971387 2014 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and anti-HIV-1 activity of the conjugates of gossypol with oligopeptides and d-glucosamine
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی (عمومی)
پیش نمایش صفحه اول مقاله
Synthesis and anti-HIV-1 activity of the conjugates of gossypol with oligopeptides and d-glucosamine
چکیده انگلیسی

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

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Chinese Chemical Letters - Volume 25, Issue 7, July 2014, Pages 1052–1056
نویسندگان
, , , , , , ,