title: Anti-HBV agents. Part 1: Synthesis of alisol A derivatives: a new class of hepatitis B virus inhibitors.
abstract: A series of alisol A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in vitro. The preliminary investigation demonstrates that simple modifications of the parent structure of alisol A can produce a number of potentially important derivatives against HBV. The most active anti-HBV compound 6a showed high activities against the secretion of HBV surface antigen (IC(50)=0.024 mM), HBV e antigen (IC(50)=0.028 mM) and remarkable selective indices (SI(HBsAg)>108, SI(HBeAg)>93), which was selected for further evaluation as a novel HBV inhibitor.
authors.affiliation: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Lanhei Road, Kunming 650204, PR China.
authors.forename: Quan
authors.initials: Q
authors.lastname: Zhang
authors.forename: Zhi-Yong
authors.initials: ZY
authors.lastname: Jiang
authors.forename: Jie
authors.initials: J
authors.lastname: Luo
authors.forename: Pi
authors.initials: P
authors.lastname: Cheng
authors.forename: Yun-Bao
authors.initials: YB
authors.lastname: Ma
authors.forename: Xue-Mei
authors.initials: XM
authors.lastname: Zhang
authors.forename: Feng-Xue
authors.initials: FX
authors.lastname: Zhang
authors.forename: Jun
authors.initials: J
authors.lastname: Zhou
authors.forename: Ji-Jun
authors.initials: JJ
authors.lastname: Chen
mesh_terms: D000956:Antigens, Viral / Q000737:chemistry; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002783:Cholestenones / Q000138:chemical synthesis* / Q000737:chemistry; D004279:DNA, Viral; D015195:Drug Design; D006509:Hepatitis B / Q000188:drug therapy*; D006511:Hepatitis B Antigens / Q000276:immunology; D006515:Hepatitis B virus / Q000378:metabolism*; D006801:Humans; D017665:Hydroxyl Radical; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000956:Antigens, Viral; D000998:Antiviral Agents; D002783:Cholestenones; D004279:DNA, Viral; D006511:Hepatitis B Antigens; C000050:alisol A; D017665:Hydroxyl Radical