Ten novel bisamides compounds containing benzothiazol unit were synthesized. Their structures were characterized by 1H NMR, 13C NMR, IR and elemental analyses. Preliminary bioassay indicated that some compounds posed antitumor activity to PC3 and BGC-823 cells in vitro by MTT method. The antiproliferation activity of compound N-(2-(6-methylbenzothiazol-2-ylcarbamoyl)4-methylphenyl)-4-chlorobenzenecarboxamide (4a) and N-(2-(4-methylbenzothiazol -2-ylcarbamoyl)-4-methylphenyl)-2-methylbenzene carboxamide (4e) to PC3 cells at the concentration of 10 μmol•L-1 was 70.8% and 68.4%. And the antiproliferation activity of compound N-(2-(benzothiazol-2-ylcarbamoyl)-4-methylphenyl)-2-methylbenzenecarboxamide(4d) to BGC-823 cells at the concentration of 10 μmol•L-1 was 65.9%.