Twenty-three (E)-4-(3-(2-bromophenyl) acryyl) phenyl - substituted benzenesulfonic ester derivatives were designed and synthesized based on the pharmacophore combination principle (yield: 60.9 to 80.3%), and their structures were confirmed by 1H NMR, MS and 13C NMR. The in vitro antitumor activity of the target compound was evaluated by MTT assay using 5-fluorouracil and imatinib as positive control, human cervical cancer Hela cells, human lung cancer A549 cells and human chronic myelocytic leukemia K562 cells as test cell lines. Target compound Vp exhibited the strongest A549 cell proliferation inhibitory activity (IC50 = 7.53 μmol/L), better than the positive control drug 5-fluorouracil (IC50 = 8.1 μmol/L), target compound Vt exhibited the strongest inhibitory activity of K562 cell proliferation inhibition (IC50 = 4.47 μmol/L), target compound Vd exhibited the strongest Hela cell proliferation inhibitory activity (IC50 = 4.53 μmol/L), than positive control drug 5-fluorouracil (IC50 = 13.5 μmol/L) is approximately 3 times stronger, and the target compound Vd also exhibits strong proliferation inhibitory activity against A549 cells (IC50 = 8.0 μmol/L) and K562 cells (IC50 = 7.81 μmol/L), which deserves further study.