1. Academic Validation
  2. Synthesis and in vitro anti-hepatitis B virus activity of 6H-[1]benzothiopyrano[4,3-b]quinolin-9-ols

Synthesis and in vitro anti-hepatitis B virus activity of 6H-[1]benzothiopyrano[4,3-b]quinolin-9-ols

  • Bioorg Med Chem. 2009 Jul 1;17(13):4569-74. doi: 10.1016/j.bmc.2009.05.001.
Wei Jia 1 Yajing Liu Wei Li Yan Liu Dajun Zhang Peng Zhang Ping Gong
Affiliations

Affiliation

  • 1 Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenhe District, Shenyang, Liaoning, PR China.
Abstract

A series of novel 6H-[1]benzothiopyrano[4,3-b]quinoline derivatives were prepared and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in human hepatoblastoma-derived liver Hep-G2 cells. Compounds 10g, 10h, 10j, 10l and 10o were found to be potent anti-HBV compounds with IC(50) values less than 50 microM. The most promising compound was 10l, with an IC(50) value of 14.7 microM and a SI value of 12.4. This is the first report of the anti-HBV effects of 6H-[1]benzothiopyrano[4,3-b] quinolin-9-ols.

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