Synthesis, biological evaluation and structure-activity relationships of glycyrrhetinic acid derivatives as novel anti-hepatitis B virus agents

  • Bioorg Med Chem Lett. 2012 May 15;22(10):3473-9. doi: 10.1016/j.bmcl.2012.03.081.
Li-Jun Wang  1 ,  Chang-An Geng ,  Yun-Bao Ma ,  Xiao-Yan Huang ,  Jie Luo ,  Hao Chen ,  Xue-Mei Zhang ,  Ji-Jun Chen
Affiliations
  • 1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China.
PMID: 22520261 DOI: 10.1016/j.bmcl.2012.03.081
Abstract

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 IC(50) values of 5.71, 5.36, 8.90 and 9.08 μM, respectively. The structure-activity relationships (SARs) of GA derivatives were discussed for exploring novel anti-HBV agents.