title: Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus.
abstract: A series of novel benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compound 12a, with IC50<0.41 microM and SI>81.2, was the most promising compound and selected as the benchmark compound for further optimization.
authors.affiliation: Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Luo
authors.forename: Jia-Ping
authors.initials: JP
authors.lastname: Yao
authors.forename: Li
authors.initials: L
authors.lastname: Yang
authors.forename: Chun-Lan
authors.initials: CL
authors.lastname: Feng
authors.forename: Wei
authors.initials: W
authors.lastname: Tang
authors.forename: Gui-Feng
authors.initials: GF
authors.lastname: Wang
authors.forename: Jian-Pin
authors.initials: JP
authors.lastname: Zuo
authors.forename: Wei
authors.initials: W
authors.lastname: Lu
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006509:Hepatitis B / Q000188:drug therapy*; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D001562:Benzimidazoles