Synthesis and in vitro anti-hepatitis B virus activities of some ethyl 5-hydroxy-1H-indole-3-carboxylates

A series of ethyl 5-hydroxy-1H-indole-3-carboxylates 6A–10T were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The IC50 and selective index of inhibition on replication of HBV DNA of compounds 10L (1.52 μg/ml, 9.38) and 10P (2.00 μg/ml, 8.85) were higher than those of the other evaluated compounds including lamivudine (7.02). Compounds 7E and 10J exhibited significant anti-HBV activities, and the IC50 values on replication of HBV DNA of these compounds were 24.90 and 15.41 μg/ml, respectively, which were far more potent than the positive control lamivudine 228.00 μg/ml.

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