Fluorinated betulinic acid derivatives and evaluation of their anti-HIV activity.
Journal Article (Journal Article)
Several fluorinated derivatives of the anti-HIV maturation agent bevirimat (1) were synthesized and evaluated for anti-HIV replication activity. The modified positions were the C-2, C-3, C-28, and C-30 positions, either directly on the betulinic acid (2) skeleton or in the attached side chains. Compound 18, which has a trifluoromethyl group added to C-30 of its isopropenyl group, exhibited similar potency to 1 against HIV-1NL4-3. In total, our current studies support our prior conclusion that C-30 allylic modification is unlikely to be a pharmacophore for anti-HIV activity, but could be a meaningful route to manipulate other properties of 2-related compounds.
- Li, J; Goto, M; Yang, X; Morris-Natschke, SL; Huang, L; Chen, C-H; Lee, K-H
- January 1, 2016
Volume / Issue
- 26 / 1
Start / End Page
- 68 - 71
Pubmed Central ID
Electronic International Standard Serial Number (EISSN)
Digital Object Identifier (DOI)