Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry.
Published
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
Language
- eng
Conference Location
- England