Chemical Research in Chinese Universities ›› 2014, Vol. 30 ›› Issue (6): 937-940.doi: 10.1007/s40242-014-4240-6

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Syntheses and Anti-cancer Activities of Derivatives of Tetrandrine and Fangchinoline

LIU Yazhou1,2, HUANG Lan1, SUN Qianyun1, ZHANG Maosheng1, LI Tianlei1, LIANG Guangyi1, PAN Weidong1   

  1. 1. Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002, P. R. China;
    2. School of Pharmaceutical Sciences, Guizhou University, Guiyang 55000, P. R. China
  • Received:2014-06-27 Revised:2014-09-04 Online:2014-12-01 Published:2014-09-15
  • Contact: LIANG Guangyi, PAN Weidong E-mail:guangyi_liang@126.com;wdpan@163.com
  • Supported by:

    Supported by the National Natural Science Foundation of China(No.81360479), the Ministry of Science and Technology of China(No.2012CB722601) and the Science and Technology Department of Guizhou Province, China(Nos.QKHZYZ[2011]5085, QKHRZ[2011]33).

Abstract:

A series of derivatives of tetrandrine and fangchinoline was designed and synthesized to find more active anti-cancer compounds. Their anti-cancer activities were tested against human hepatocellular carcinoma BEL-7402 and PLC/PRF/5 cells, human lung adenocarcinoma A549 cells as well as human leukaemia K562 cells, and the structure-activity relationship(SAR) was also studied. All the compounds except B1 exhibited superior inhibitory activities against PLC/PRF/5 cells with half maximal inhibitory concentration(IC50) values of less than 15 μmol/L, and compounds A2, A4, B2 and B4 showed IC50 values of less than 9 μmol/L. Compounds A2, A6, B2 and B4 showed potent anti-cancer activities against all the tested cells with IC50 values of less than 10 μmol/L. The results show that terandrine and fangchinoline derivatives are potential suppressors to human cancer.

Key words: Tetrandrine, Fangchinoline, Derivative, Cytotoxicity