title: Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents.
abstract: A series of 4-aryl-6-chloro-quinoline derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities, namely the abilities to inhibit the secretion of HBV surface antigen (HBsAg), HBV e antigen (HBeAg), and replication of HBV DNA in HepG 2.2.15 cells. Most of the compounds exhibited moderate inhibitory activity against the secretion of HBsAg and HBeAg. Nine compounds (3, 5, 6, 7, 10, 14, 17, 20, 24) showed significant inhibition against HBV DNA replication with IC(50) values in the range of 4.4-9.8 μM, which were comparative to that of positive control tenofovir. Of them, compounds 10, 17, and 20 had low cytotoxicities, resulting in high SI values, >551.2, >143.7, and >284.5, respectively.
authors.affiliation: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, PR China.
authors.forename: Rui-Hua
authors.initials: RH
authors.lastname: Guo
authors.forename: Quan
authors.initials: Q
authors.lastname: Zhang
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: Li-Jun
authors.initials: LJ
authors.lastname: Wang
authors.forename: Chang-An
authors.initials: CA
authors.lastname: Geng
authors.forename: Xue-Mei
authors.initials: XM
authors.lastname: Zhang
authors.forename: Jun
authors.initials: J
authors.lastname: Zhou
authors.forename: Zhi-Yong
authors.initials: ZY
authors.lastname: Jiang
authors.forename: Ji-Jun
authors.initials: JJ
authors.lastname: Chen
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D004261:DNA Replication / Q000187:drug effects; D004279:DNA, Viral / Q000378:metabolism; D006515:Hepatitis B virus / Q000187:drug effects* / Q000378:metabolism; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D004279:DNA, Viral; D011804:Quinolines