title: Synthesis, biological evaluation and structure-activity relationships of glycyrrhetinic acid derivatives as novel anti-hepatitis B virus agents.
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.
authors.affiliation: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China.
authors.forename: Li-Jun
authors.initials: LJ
authors.lastname: Wang
authors.forename: Chang-An
authors.initials: CA
authors.lastname: Geng
authors.forename: Yun-Bao
authors.initials: YB
authors.lastname: Ma
authors.forename: Xiao-Yan
authors.initials: XY
authors.lastname: Huang
authors.forename: Jie
authors.initials: J
authors.lastname: Luo
authors.forename: Hao
authors.initials: H
authors.lastname: Chen
authors.forename: Xue-Mei
authors.initials: XM
authors.lastname: Zhang
authors.forename: Ji-Jun
authors.initials: JJ
authors.lastname: Chen
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004261:DNA Replication / Q000187:drug effects; D004279:DNA, Viral / Q000096:biosynthesis / Q000187:drug effects; D006034:Glycyrrhetinic Acid / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006515:Hepatitis B virus / Q000187:drug effects* / Q000235:genetics / Q000502:physiology; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D004279:DNA, Viral; D006034:Glycyrrhetinic Acid