Novel Betulinic Acid–Nucleoside Hybrids with Potent Anti-HIV Activity
Qiang Wang, Yujiang Li, Liyun Zheng, Xiaowan Huang, Yanli Wang, Chin‐Ho Chen, Yung‐Yi Cheng, Susan L. Morris‐Natschke, Kuo‐Hsiung Lee
Abstract
Novel betulinic/betulonic acid–nucleoside hybrids were synthesized as possible new anti-HIV agents. Among the synthesized hybrids, two compounds were highly effective against HIV. Compared with AZT and DSB, compounds 10a (IC50 = 0.0078 μM, CC50 = 9.6 μM) and 10b (IC50 = 0.020 μM, CC50 = 23.8 μM) showed more potent or equipotent, respectively, anti-HIV activity but displayed lower cytotoxicity.
Topics & Concepts
Betulinic acidCytotoxicityHuman immunodeficiency virus (HIV)IC50HybridNucleosideChemistryTenofovirStereochemistryIn vitroBiologyBiochemistryVirologyGeneticsBotanyNatural product bioactivities and synthesisPlant biochemistry and biosynthesisPhytochemical compounds biological activities