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

Identifieur interne : 001C46 ( Main/Exploration ); précédent : 001C45; suivant : 001C47

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 ; Yun-Bao Ma ; Xiao-Yan Huang ; Jie Luo ; Hao Chen ; Xue-Mei Zhang ; Ji-Jun Chen

Source :

RBID : pubmed:22520261

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 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.

DOI: 10.1016/j.bmcl.2012.03.081
PubMed: 22520261


Affiliations:


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Le document en format XML

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<term>DNA, Viral (biosynthesis)</term>
<term>DNA, Viral (drug effects)</term>
<term>Glycyrrhetinic Acid (chemical synthesis)</term>
<term>Glycyrrhetinic Acid (chemistry)</term>
<term>Glycyrrhetinic Acid (pharmacology)</term>
<term>Hepatitis B virus (drug effects)</term>
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<term>Relation structure-activité</term>
<term>Réplication de l'ADN ()</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(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.</div>
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