Synthesis and in vitro anti-hepatitis B virus activity of 6H-[1]benzothiopyrano[4,3-b]quinolin-9-ols |
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| Authors: | Wei Jia Yajing Liu Wei Li Yan Liu Dajun Zhang Peng Zhang Ping Gong |
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| Institution: | Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, Liaoning 110016, PR China |
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| Abstract: | A series of novel 6H-1]benzothiopyrano4,3-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 IC50 values less than 50 μM. The most promising compound was 10l, with an IC50 value of 14.7 μM and a SI value of 12.4. This is the first report of the anti-HBV effects of 6H-1]benzothiopyrano4,3-b] quinolin-9-ols. |
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