Abstract: Eight Mono-carbonyl curcumin analogues were synthesized by three-step reaction of alkylation, hydroxyl protection, aldehyde ketone condensation. Their structures were characterized by 1H NMR and ESI-MS techniques. Then all the compounds were synthesized and evaluated for their effects on cultured prostate cancer PC-3 cells, pancreas cancer BxPC-3 cells, colon cancer HT-29 cells and lung cancer H1299 cells. These compounds exhibited potent inhibitory effects on the growth of cultured PC-3, BxPC-3, HT-29 and H1299 cells. The IC50 for A6 was lower than 0.65μM in all four cell lines, and A6 was 40-fold more active than curcumin.