title: Synthesis and Anti-Hepatitis B Virus Evaluation of 7-Methoxy-3-heterocyclic quinolin-6-ols.
abstract: A series of novel 7-methoxy-3-heterocyclic quinolin-6-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in the HepG2.2.15 cell line. Five compounds, 14a, 15c, 15e, 16b, and 16f, displayed excellent potency and selectivity toward the HBV, with IC50values of less than 5.0 µM and selectivity index values of 11.0-71.5. Structure-activity relationship studies indicated that the 1,3,4-thiadiazole and sulfinylmethyl derivatives showed the most potent activities against the HBV.
authors.affiliation: Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, P. R. China.
authors.forename: Yajing
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, P. R. China.
authors.forename: Guobing
authors.initials: G
authors.lastname: Feng
authors.affiliation: Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, P. R. China.
authors.forename: Zonghui
authors.initials: Z
authors.lastname: Ma
authors.affiliation: Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, P. R. China.
authors.forename: Chen
authors.initials: C
authors.lastname: Xu
authors.affiliation: Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, P. R. China.
authors.forename: Zhuang
authors.initials: Z
authors.lastname: Guo
authors.affiliation: Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, P. R. China.
authors.forename: Ping
authors.initials: P
authors.lastname: Gong
authors.affiliation: Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, P. R. China.
authors.forename: Liying
authors.initials: L
authors.lastname: Xu
keywords: 3-Heterocyclic-6-hydroxyquinolines; Hepatitis B virus; Synthesis