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 IC50 values less than 50μM. The most promising compound was 10l, with an IC50 value of 14.7 μM and a SI value of 12.4. This ...