高等学校化学研究 ›› 2010, Vol. 26 ›› Issue (2): 272-277.
Synthesis and in vitro Anti-hepatitis B Virus Activity of Some Ethyl 5-Hydroxy-4-substituted Aminomethyl-2-sulfinylmethyl-1H-indole-3-carboxylates
ZHAO Yan-fang1, FENG Run-liang2, LIU Ya-jing1, ZHANG Yi-kun1 and GONG Ping1*
- 1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China;
2. School of Medical and Life Science, University of Jinan, Jinan 250022, P. R. China
Synthesis and in vitro Anti-hepatitis B Virus Activity of Some Ethyl 5-Hydroxy-4-substituted Aminomethyl-2-sulfinylmethyl-1H-indole-3-carboxylates
ZHAO Yan-fang1, FENG Run-liang2, LIU Ya-jing1, ZHANG Yi-kun1 and GONG Ping1*
- 1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China;
2. School of Medical and Life Science, University of Jinan, Jinan 250022, P. R. China
摘要：
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).