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《高等学校化学研究:英文版》
>Synthesis and in vitro Anti-hepatitis B Virus Activity of Some Ethyl 5-Hydroxy-4-substituted Aminomethyl-2-sulfinylmethyl-1H-indole-3-carboxylates
Synthesis and in vitro Anti-hepatitis B Virus Activity of Some Ethyl 5-Hydroxy-4-substituted Aminomethyl-2-sulfinylmethyl-1H-indole-3-carboxylates
A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-1H-indole-3-carboxylates 8a―8j and 11e―11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus(HBV) acti-vity and cytotoxicity.Among them,six compounds showed more potent inhibitory activity than lamivudine.Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L,which was 33-times more potent than the reference drug lamivudine(IC50=54.78 μmol/L).
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