title: Synthesis and biological evaluation of 1H-benzimidazol-5-ols as potent HBV inhibitors.
abstract: A new series of 1-methyl-1H-benzimidazol-5-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. Some of the analogues in this series displayed inhibitory activity superior to lamivudine. Of them, compound 13b was the most potent one, showing an IC(50) value of 7.8 μM and a SI value of 13.0.
authors.affiliation: Key Lab of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, PR China.
authors.forename: Yanfang
authors.initials: Y
authors.lastname: Zhao
authors.forename: Yajing
authors.initials: Y
authors.lastname: Liu
authors.forename: Dong
authors.initials: D
authors.lastname: Chen
authors.forename: Zengquan
authors.initials: Z
authors.lastname: Wei
authors.forename: Wenzhao
authors.initials: W
authors.lastname: Liu
authors.forename: Ping
authors.initials: P
authors.lastname: Gong
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D045744:Cell Line, Tumor; D004261:DNA Replication / Q000187:drug effects; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D019259:Lamivudine / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D001562:Benzimidazoles; D019259:Lamivudine