Fifty-seven derivatives of glycyrrhetinic acid (GA) were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Among them, sixteen compounds showed greater anti-HBV activity than GA, especially, compounds 29, 32, 35, 41 exhibited significantly inhibitory activities against HBV DNA replication with IC50 values of 5.71, 5.36, 8.90 and 9.08 mu M, respectively. The structure-activity relationships (SARs) of GA derivatives were discussed for exploring novel anti-HBV agents. (C) 2012 Elsevier Ltd. All rights reserved.
1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650201, Peoples R China 2.Chinese Acad Sci, Grad Univ, Beijing 100049, Peoples R China
Recommended Citation:
Wang, LJ; Geng, CA; Ma, YB; Huang, XY; Luo, J; Chen, H; Zhang, XM; Chen, JJ.Synthesis, biological evaluation and structure-activity relationships of glycyrrhetinic acid derivatives as novel anti-hepatitis B virus agents,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(10):3473-3479
