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

作　　者：LIU Yazhou HUANG Lan SUN Qianyun ZHANG Maosheng LI Tianlei LIANG Guangyi PAN Weidong 

机构地区：[1]Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guivang 550002, P. R. China," [2]School of Pharmaceutical Sciences, Guizhou University, Guiyang 55000, P. R. China

出　　处：《Chemical Research in Chinese Universities》2014年第6期937-940,共4页高等学校化学研究（英文版）

基　　金：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）.

摘　　要：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 hcpatocellular 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 BI exhibited superior inhibitory ac- tivities against PLC/PRF/5 cells with half maximal inhibitory conccntration（ICs0） values of less than 15 μmol/L, and compounds A2, A4, B2 and B4 showed IC50 values of less than 9 pmol/L. Compounds A2, A6, B2 and B4 showed potent anti-cancer activities against all the tested cells with 1C5o values of less than 10 pmol/L. The results show that terandrine and fangchinoline derivatives are potential suppressors to human cancer.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 hcpatocellular 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 BI exhibited superior inhibitory ac- tivities against PLC/PRF/5 cells with half maximal inhibitory conccntration（ICs0） values of less than 15 μmol/L, and compounds A2, A4, B2 and B4 showed IC50 values of less than 9 pmol/L. Compounds A2, A6, B2 and B4 showed potent anti-cancer activities against all the tested cells with 1C5o values of less than 10 pmol/L. The results show that terandrine and fangchinoline derivatives are potential suppressors to human cancer.

关 键 词：TETRANDRINE FANGCHINOLINE DERIVATIVE CYTOTOXICITY 

分 类 号：Q255[生物学—细胞生物学] O627.42[理学—有机化学]