Objective: To study the synthesis and in vitro anti-cancer activity of new curcumin derivatives. Method: Three new curcumin derivatives were synthesized using anti-tumor ingredients of Shiquandabu Wan as starting materials. Our idea was enlightened by the ‘combination principle’ in drug discovery. The curcumin derivatives anti-tumor activities were evaluated on the HT-29

Bel-7402

HepG2 and Hela human cancer cell lines and their toxicities were evaluated on MDCK (madin-darby canine kidney cell lines). Result: Compound 4 and CU-T displayed more antiproliferative activities on these cancer cells than their starting materials; IC50 values were similar to DDP's

while curcumin derivatives showed much lower toxicity on MDCK cell than DDP. Conclusion: It is feasible to discover high-effect and low-toxicity lead compounds from classic formulas via combination principle.