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

Identifieur interne : 001F60 ( Main/Exploration ); précédent : 001F59; suivant : 001F61

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

Auteurs : Li-Jun Wang [République populaire de Chine] ; Chang-An Geng [République populaire de Chine] ; Yun-Bao Ma [République populaire de Chine] ; Xiao-Yan Huang [République populaire de Chine] ; JIE LUO [République populaire de Chine] ; HAO CHEN [République populaire de Chine] ; Xue-Mei Zhang [République populaire de Chine] ; Ji-Jun Chen [République populaire de Chine]

Source :

RBID : Pascal:12-0355115

Descripteurs français

English descriptors

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 IC50 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.


Affiliations:


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<term>Hepatitis B virus</term>
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<div type="abstract" xml:lang="en">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
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