Nine novel resveratrol derivatives were synthesized from resveratrol, chloroacetyl chloride, p-toluenesulfonyl chloride and p-methyl benzoyl chloride. These structures were confirmed by IR. H-1 NMR, C-13 NMR and HR-MS techniques. The target compounds were evaluated for their anti-tumor activities against cervical cancer HeLa cells by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method, and the results indicated that compounds 4a, 6a, 7b, 8b and 11c of all the derivatives displayed better activities than resveratrol against HeLa cells, the compounds 6a and 8b displayed excellent inhibition effect, with IC50 values of 22.7 and 18.0 [anon, respectively, even higher than that of resveratrol (IC50=114 mu mol/L). The inhibitory ratio of compounds 6a and 8b were 95.5% and 87.7% against HeLa cells at the concentration of 150 mu mol/L.