A binaphthyl-linked bipyridyl compound, 1,1'-bis(6-methyl-6'-oxymethylenyl-2,2'-bipyridine)binaphthyl, (L) has been synthesised and used as a ligand for the formation of Cu(II), Ni(II), and Co(II) complexes. The ligand and its transition-metal complexes were characterized by physico-chemical and spectroscopic methods. The complexes were also investigated for cytotoxic activity. The cytotoxicity of complexes, CuL(ClO(4))(2), NiL(ClO(4))(2)(H(2)O), CoL(ClO(4))(2), were tested in vitro applying seven well-characterized human tumor cell lines, MCF7, EVSA-T, WIDR, IGROV, M19 MEL, A498, H226, and the microculture sulforhodamine B (SRB) test. All complexes show a very high cytotoxicity (ID(50) < 250 ng/ml) in these cell lines.