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

Journal Article (Journal Article)

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 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.

Full Text

Duke Authors

Cited Authors

  • Bori, ID; Hung, H-Y; Qian, K; Chen, C-H; Morris-Natschke, SL; Lee, K-H

Published Date

  • April 11, 2012

Published In

Volume / Issue

  • 53 / 15

Start / End Page

  • 1987 - 1989

PubMed ID

  • 22711941

Pubmed Central ID

  • 22711941

International Standard Serial Number (ISSN)

  • 0040-4039

Digital Object Identifier (DOI)

  • 10.1016/j.tetlet.2012.02.022


  • eng

Conference Location

  • England