2. Academic Validation
  3. Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents

Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents

  • Bioorg Med Chem. 2011 Feb 15;19(4):1400-8. doi: 10.1016/j.bmc.2011.01.006.
Rui-Hua Guo 1,  Quan Zhang,  Yun-Bao Ma,  Xiao-Yan Huang,  Jie Luo,  Li-Jun Wang,  Chang-An Geng,  Xue-Mei Zhang,  Jun Zhou,  Zhi-Yong Jiang,  Ji-Jun Chen
Affiliations

Affiliation

  • 1 State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, PR China.
PMID: 21292495 DOI: 10.1016/j.bmc.2011.01.006
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.

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