Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 10, Pages 3473-3479Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.03.081
Keywords
Glycyrrhetinic acid derivatives; Anti-HBV activity; Structure-activity relationships
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Funding
- National Natural Science Foundation of China for Distinguished Young Scholars [81025023]
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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.
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