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

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.