A series of novel N-(5-benzyl-4-(tert-butyl) thiazol-2-yl)-2-(piperazin-1yl) acetamides were designed, synthesized and evaluated for their antitumor activities in vitro. The structures of the synthesized compounds were characterized by H-1 NMR, C-13 NMR and elemental analysis. In general, compounds 5a, 5c and 6a showed potent antiproliferative activity against HeLa (human cervical cancer) and A549 (human lung cancer) cell lines. Compound 6a, with the best inhibitory activity against HeLa cells (IC50 = 1.6 +/- 0.8 mu M), was selected to investigate the induced changes of cell morphology in the ...