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.
MeSH terms
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Antiviral Agents / chemical synthesis
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Antiviral Agents / chemistry*
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Antiviral Agents / pharmacology*
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Antiviral Agents / toxicity
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Cell Line, Tumor
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Cell Survival / drug effects*
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DNA, Viral / analysis
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DNA, Viral / metabolism
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Hepatitis B Surface Antigens / analysis
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Hepatitis B Surface Antigens / metabolism
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Hepatitis B virus / drug effects*
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Hepatitis B virus / physiology
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Humans
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Inhibitory Concentration 50
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Liver / cytology
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Microbial Sensitivity Tests
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Quinolines / chemical synthesis
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Quinolines / chemistry*
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Quinolines / pharmacology*
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Quinolines / toxicity
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Structure-Activity Relationship
Substances
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Antiviral Agents
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DNA, Viral
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Hepatitis B Surface Antigens
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Quinolines