Chemical Research in Chinese Universities ›› 2010, Vol. 26 ›› Issue (2): 272-277.

• Articles • Previous Articles     Next Articles

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. 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
  • Received:2009-02-23 Revised:2009-04-03 Online:2010-03-25 Published:2010-05-25
  • Contact: GONG Ping. E-mail: gongpinggp@126.com
  • Supported by:

    Supported by the National Natural Science Foundation of China(No.30672519).

Abstract:

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).

Key words: 5-Hydroxy-2-sulfinylmethyl-1H-indole-3-carboxylates; Anti-hepatitis B virus activity; Synthesis