A new nickel(II) complex with 5,7-dichloro-8-hydroxylquinoline (H-ClQ), [NiCl(ClQ)(H-ClQ)(mu-Cl)Ni(ClQ)(CH3CH2OH)(H-ClQ)]center dot CH3COCH3 (1), was synthesized and characterized. In solid state, 1 is consisted of a dinuclear nickel(II) complex and one acetone solvent molecule. Two Ni(II) atoms are chelated by two bidentate 5,7-dichloro-8-hydroxylquinolines and coordinated by one terminal Cl atom or ethanol ligand and one mu-Cl in a distorted octahedral coordination environment. The ESI-MS result shows that the mu-Cl bridge is easily broken in solution to give mononuclear species (omitted as ClQ-Ni complex). The IC50 values of 1 for the inhibition of the proliferation of BEL7404, SGC7901 and MCF-7 tumor cells are 13.0 +/- 2.1, 15.9 +/- 5.3, and 29.8 +/- 9.5 mu M, respectively, which exhibit significantly enhanced cytotoxicity comparing with free H-ClQ and NiCl2. The binding properties of ClQ-Ni complex to DNA were investigated by UV-Vis, fluorescence, CD spectroscopy, viscosity and agarose gel electrophoresis. The results indicate that intercalation is the most probable binding mode for ClQ-Ni complex to DNA. The ClQ-Ni complex exhibits potent TOPO I inhibition activity at 50 mu M. (C) 2011 Elsevier B. V. All rights reserved.