Conjugates of betulin derivatives with AZT as potent anti-HIV agents.

Journal Article (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

  • PMC3016297

Electronic International Standard Serial Number (EISSN)

  • 1464-3391

Digital Object Identifier (DOI)

  • 10.1016/j.bmc.2010.06.092

Language

  • eng

Conference Location

  • England