Conjugates of betulin derivatives with AZT as potent anti-HIV agents.
Journal Article
Fourteen novel conjugates of 3,28-di-O-acylbetulins with AZT were prepared as anti-HIV agents, based on our previously reported potent anti-HIV triterpene leads, including 3-O-acyl and 3,28-di-O-acylbetulins. Nine of the conjugates (49-53, 55, 56, 59, and 60) exhibited potent anti-HIV activity at the submicromolar level, with EC(50) values ranging from 0.040 to 0.098muM in HIV-1(NL4-3) infected MT-4 cells. These compounds were equipotent or more potent than 3-O-(3',3'-dimethylsuccinyl)betulinic acid (2), which is currently in Phase IIb anti-AIDS clinical trial.
Full Text
Duke Authors
Cited Authors
- Xiong, J; Kashiwada, Y; Chen, C-H; Qian, K; Morris-Natschke, SL; Lee, K-H; Takaishi, Y
Published Date
- September 1, 2010
Published In
Volume / Issue
- 18 / 17
Start / End Page
- 6451 - 6469
PubMed ID
- 20673723
Pubmed Central ID
- 20673723
Electronic International Standard Serial Number (EISSN)
- 1464-3391
Digital Object Identifier (DOI)
- 10.1016/j.bmc.2010.06.092
Language
- eng
Conference Location
- England