Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry

Ibrahim D. Bori, Hsin Yi Hung, Keduo Qian, Chin Ho Chen, Susan L. Morris-Natschke, Kuo Hsiung Lee

研究成果: Article同行評審

69 引文 斯高帕斯(Scopus)

摘要

In the present study, a new strategy to link AZT with betulin/betulinic acid (BA) by click chemistry was designed and achieved. This conjugation via a triazole linkage offers a new direction for the modification of anti-HIV triterpenes. Click chemistry provides an easy and productive way for linking two molecules, even when one of them is a large natural product. Among the newly synthesized conjugates, compounds 15 and 16 showed potent anti-HIV activity with EC 50 values of 0.067 and 0.10 μM, respectively, which are comparable to that of AZT (EC 50: 0.10 μM) in the same assay.

原文English
頁(從 - 到)1987-1989
頁數3
期刊Tetrahedron Letters
53
發行號15
DOIs
出版狀態Published - 2012 4月 11

All Science Journal Classification (ASJC) codes

  • 生物化學
  • 藥物發現
  • 有機化學

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