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

Authors :: Wang LJ
Geng CA
Ma YB
Huang XY
Luo J
Chen H
Zhang XM
Chen JJ
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 May 15; Vol. 22 (10), pp. 3473-9. Date of Electronic Publication: 2012 Mar 28.
Publication Year :: 2012
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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Subjects :: Antiviral Agents chemistry
DNA Replication drug effects
DNA, Viral biosynthesis
DNA, Viral drug effects
Glycyrrhetinic Acid chemistry
Hepatitis B virus genetics
Hepatitis B virus physiology
Structure-Activity Relationship
Virus Replication drug effects
Antiviral Agents chemical synthesis
Antiviral Agents pharmacology
Glycyrrhetinic Acid chemical synthesis
Glycyrrhetinic Acid pharmacology
Hepatitis B virus drug effects

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