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A series of ethyl 5-hydroxyindole-3-carboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, 1H NMR, and MS and their anti-hepatitis B virus(HBV) activities were evaluated in 2.2.15 cells. Among them, compound 7g {ethyl 5-hydroxy-2-[(3-methoxyphenylsulfinyl) methyl] -1-methyl-4-[ (4-methylpiperazin-1-yl)methyl]-1H-indole-3-carboxylate} displays a significant anti-HBV activity, which is more potent than the positive control lamivudine.