A series of hydantoin derivatives were designed and synthesized about 25-30% overall yields. Two of the six newly synthesized compounds, compound 3, 5 have not been reported before. Compounds 2-6 were obtained by Aldol reaction，and those structures were confirmed by 1H and 13C NMR. All the newly synthesized derivatives were subjected to evaluate their cytotoxic properties against human tumor cell lines, HepG2. Results indicated that compounds 2 and 4 exhibited significant anti-tumor activities against liver cancer (HepG2)cell lines. Among, compound 2 with the IC50 values of 3.37 μM against cancer cell lines HepG2.