Copper(II) complexes of ethyl 2-[bis(2-pyridylmethyl)amino]propionate ligand (ETDPA) have been synthesized and characterized by elemental analyses, IR spectra, UV spectra and ES-MS. These complexes are stable in air with the formula of [(ETDPA)CuCl(2)] and [(ETDPA)Cu(phen)](ClO(4))(2). The DNA-binding properties of the Cu(II) complexes have been investigated by ultraviolet spectroscopy and fluorescence spectroscopy, which showed that the binding mode of the two complexes with DNA was different. The binding mode of [(ETDPA)CuCl(2)] is not the classical intercalation binding, and the binding mode of [(ETDPA)Cu(phen)](ClO(4))(2) with DNA is intercalation. The cytotoxic assay shows that the [(ETDPA)Cu(phen)](ClO(4))(2) is more active on the proliferation of cancer cells than the [(ETDPA)CuCl(2)].