Pinanyl thiazole hydrazone derivatives 4a~n were synthesized from nopinone via addition, condensation and cyclization, and their structures were characterized by FTIR, 1HNMR, 13CNMR and HRMS. The antitumor activities of compounds 4a~n against four human cancer cell lines including HepG2, RPMI-8226, A549 and MDA-MB-231 were evaluated in vitro. The test results showed that compounds 4a had best antitumor activity against the above four cancer cell, IC50 values for HepG2, RPMI-8226, A549 and MDA-MB-231 as low as 5.8, 8.8, 7.1 and 10.6 μmol/L, respectively; compound 4c also had stronger activity and the IC50 values was 8.9, 8.7, 7.3 and 9.7 μmol/L, respectively. Cell apoptosis and cell cycle experiments results indicated that as the concentrations of compound 4a increased from 0 to 40 μmol/L, the total apoptotic rate of A549 cells increased from 6.5% to 47.2%, and the number of cells in G2/M phase increased from 13.5% to 51.7%. The above results indicated that compound 4a effectively fuelled A549 cells apoptosis in a dose-dependent manner and arrested the cell cycle at the G2/M phase.