A series of ((4-([1,2,4]triazolo[4,3-b][1,2,4,5] methyl) benzo-hydrazide derivatives was designed, synthesized, and evaluated for their inhibition activities against five tumor cells and c-Met kinase in vitro. These compounds were fully characterized by(1)H NMR,C-13 NMR, MS, and elemental analysis. Antitumor experiments indicated that some compounds exhibited significant inhibition activities against A549 and Bewo. Especially, the IC(50)values of5f(12 mu M),5h(7.1 mu M),6a(8.4 mu M), and6d(9.2 mu M) demonstrated better antitumor activities against A549 than the positive agent cisplatin (13.3 mu M), and the IC(50)value of6a(5.2 mu M) exhibited better antitumor activity against Bewo than cisplatin (7.7 mu M).