Khatereh Abdil and Hassan Hadadzadeh

Department of Chemistry, Isfahan University of Technology, Isfahan 84156-83111, Iran

Abstract:

Medicinal inorganic chemistry is a multidisciplinary field combining elements of chemistry, pharmacology, toxicology, and biochemistry. The discovery of the cytotoxic properties of cisplatin provided enormous impetus for research into the use of metal complexes in the fight against cancer. In this study, two mononuclear copper(II) complexes, [Cu(tpy)(dppz)]2+ (1) and [Cu(tptz)2]2+ (2) (tpy = 2,2'':6'',2"-terpyridine, dppz = dipyrido[3,2-a:2′,3′-c]phenazine, tptz = 2,4,6-tris(2-pyridyl)-1,3,5-triazine), were prepared and their DNA binding was investigated by various analytical techniques (absorption spectroscopy, competitive fluorescence titration, linear dichroism, gel electrophoresis, and voltammetric techniques). The complexes show moderately strong binding propensity to DNA, presumably via an intercalation mode with the partial insertion of the planar polypyridyl ligands between the base pairs of double-stranded DNA. An invitro cell cytotoxicity assay of the complexes on human breast adenocarcinoma (MCF-7) cell line was also studied by an MTT assay and the results indicate that both of the complexes have marked antiproliferative activity with IC50 values of 4.57 µM [1] and 1.98 µM [2], which are significantly better than that observed for cisplatin (57.90 µM) under the same conditions. These results, although preliminary, are promising and may shed some light on designing new potential anticancer agents in the future.

Keywords: Copper(II) complex, Polypyridyl ligand, DNA binding, Cell cytotoxicity.