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

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• 作者：Li-Jun Wang^a ; ^b ; Chang-An Geng^a ; Yun-Bao Ma^a ; Xiao-Yan Huang^a ; Jie Luo^a ; Hao Chen^a ; ^b ; Xue-Mei Zhang^a ; Ji-Jun Chen^a ; ^{chenjj@mail.kib.ac.cn}
• 关键词：Glycyrrhetinic acid derivatives ; Anti-HBV activity ; Structure&ndash ; activity relationships
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 May, 2012
• 卷：22
• 期：10
• 页码：3473-3479
• 文件大小：5043 K

摘要

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 渭M, respectively. The structure-activity relationships (SARs) of GA derivatives were discussed for exploring novel anti-HBV agents.