A ferrocenyl ligand was prepared from condensation of 1,1'-diacetylferrocene dihydrazone with salicylaldehyde. This ligand forms 1:1 complexes with Co(II), Ni(II), Cu(II), and Zn(II) in good yield. Characterization of the ligand and complexes was carried out using infrared (IR), H-1 nuclear magnetic resonance (NMR), electronic absorption, and elemental analysis. Anticancer activity of the prepared ligand and its complexes against human breast cancer cell line MCF-7 was determined, and the results were compared with the activity of the commonly used anticancer drug cisplatin. Treatments of MCF-7 cells with gradually increasing doses (5, 10, 20, and 40 mu g/cm(3)) of the prepared complexes revealed that the activity of superoxide dismutase and the level of hydrogen peroxide were significantly increased, while the activities of catalase and glutathione peroxidase and the levels of reduced glutathione were significantly lowered compared with in MCF-7 cells harvested from control. The results suggested that the prepared compounds possess significant anticancer activity comparable to the activity of cisplatin and may be potent anticancer agents for inclusion in modern clinical trials.