Synthesis and in vitro Anti-hepatitis B Virus Activity of Some Ethyl 5-Hydroxy-4-substituted Aminomethyl-2-sulfinylmethy
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) activity and cytotoxicity.Among them,six compounds showed more potent inhibitory activity than lamivudine.Compound 8e exhibited the most significant anti-HBV activity with an IC_(50) value of 1.62μmol/L,which was 33-times more potent than the reference drug lamivudine(IC_(50)=54.78μmol/L).
作 者: ZHAO Yan-fang FENG Run-Hang LIU Ya-jing ZHANG Yi-kun GONG Ping 作者单位: ZHAO Yan-fang,LIU Ya-jing,ZHANG Yi-kun,GONG Ping(School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,P.R.China)FENG Run-Hang(School of Medical and Life Science,University of Jinan,Jinan 250022,P.R.China)
刊 名: 高等学校化学研究(英文版) ISTIC SCI 英文刊名: CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 年,卷(期): 2010 26(2) 分类号: O6 关键词: 5-Hydroxy-2-sulfinylmethyl-1H-indole-3-carboxylates Anti-hepatitis B virus activity Synthesis