Mononuclear copper(II) complex with terpyridine and an extended phenanthroline base, [Cu(tpy)(dppz)]2+: Synthesis, crystal structure, DNA binding and cytotoxicity activity

The new dipyrido[3,2-a:2',3'-c]phenazine (dppz) copper(II) complex, [Cu(tpy)(dppz)](2+), where tpy is 2,2':6',2 ''-terpyridine, has been prepared and fully characterized by spectroscopic methods and single-crystal X-ray diffraction. Its DNA binding and in vitro cytotoxicity have been also studied. The molecular structure shows a distorted trigonal bipyramidal CuN5 coordination geometry around the copper atom. The bidentate dppz ligand binds in the equatorial plane, while tpy exhibits axial-equatorial bonding. The interaction of the complex with DNA has been investigated by electronic absorption, competitive fluorescence titration, linear dichroism, voltammetric techniques and a gel electrophoresis mobility shift assay. It is proposed that the binding mode of the complex to DNA is of an intercalation nature with the planar dppz ligands located between the base pairs of double-stranded DNA. An in vitro cytotoxicity study of the complex on human breast adenocarcinoma (MCF7) cell line by an MTT assay indicates that the title complex may have the potency to act as an effective anticancer drug, with an IC50 value of 4.57 mu M (3.62-5.77). (C) 2011 Elsevier Ltd. All rights reserved.