title: Synthesis and anti-hepatitis B virus activity of novel benzimidazole derivatives.
abstract: A series of novel benzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in vitro. Strong activity against HBV replication and low cytotoxicity were generally observed in these benzimidazoles. The most promising compounds were 12a and 12b, with similar high antiviral potency (IC50 = 0.9 and 0.7 microM, respectively) and remarkable selectivity indices (>1111 and 714, respectively). They were selected for further evaluation as novel HBV inhibitors.
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, 555 Zuchongzhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
authors.forename: Yun-Fei
authors.initials: YF
authors.lastname: Li
authors.forename: Gui-Feng
authors.initials: GF
authors.lastname: Wang
authors.forename: Pei-Lan
authors.initials: PL
authors.lastname: He
authors.forename: Wei-Gang
authors.initials: WG
authors.lastname: Huang
authors.forename: Feng-Hua
authors.initials: FH
authors.lastname: Zhu
authors.forename: He-Yong
authors.initials: HY
authors.lastname: Gao
authors.forename: Wei
authors.initials: W
authors.lastname: Tang
authors.forename: Yu
authors.initials: Y
authors.lastname: Luo
authors.forename: Chun-Lan
authors.initials: CL
authors.lastname: Feng
authors.forename: Li-Ping
authors.initials: LP
authors.lastname: Shi
authors.forename: Yu-Dan
authors.initials: YD
authors.lastname: Ren
authors.forename: Wei
authors.initials: W
authors.lastname: Lu
authors.forename: Jian-Ping
authors.initials: JP
authors.lastname: Zuo
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004279:DNA, Viral / Q000037:antagonists & inhibitors; D006515:Hepatitis B virus / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D001562:Benzimidazoles; D004279:DNA, Viral