In order to find efficient anti-tumor active molecules,N-(aminosulfonyl)-4-dehydroabietyl carbamates compounds were synthesized from dehydroabietic acid via 3 step reaction and their structures were confirmed by FT-IR, 1HNMR,13CNMR, and ESI-MS. The antitumor activity against T-24, HepG2, MCF-7, MGC-803 and Hela tumor cell lines was evaluated using 5-fluorouracil as positive control. The results showed that the antitumor activity of some compounds was better than that of positive drugs, and compound IVd N-((2-bromophenyl) sulfamyl) -4-dehydroabietyl carbamate showed the best activity against T-24 cell line with IC50 value of 14.64±0.46μmol/L. The primary mechanism was studied by Hoechst 33258 staining, cell colony formation, cell cycle distribution, as well as cell apoptosis and western blotting. The results showed compounds IVd significantly inhibited the growth of T-24 cells and arrested the cell cycle in the S phase. In addition, it could promote T-24 cancer cells apoptosis through upregulation of proapoptotic ones Bax and downregulation of antiapoptotic protein Bcl-2 expression. It is evident that the introduction of sulfanilamide can improve the anti-tumor activity of dehydroabietic acid, which is worthy of further study.