trans-Dichloridopalladium(II) and platinum(II) complexes with 2-(hydroxymethyl)pyridine and 2-(2-hydroxyethyl)pyridine: Synthesis, structural characterization, DNA binding and in vitro cytotoxicity studies

Icsel C., YILMAZ V. T., ARI F., Ulukaya E., Harrison W. T. A.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol.60, pp.386-394, 2013 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 60
  • Publication Date: 2013
  • Doi Number: 10.1016/j.ejmech.2012.12.002
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.386-394
  • Keywords: Transplatinum complexes, 2-(Hydroxymethyl)pyridine, 2-(2-Hydroxyethyl)pyridine, DNA binding, Cytotoxic activity, TRANS GEOMETRY, ETHIDIUM-BROMIDE, METAL-COMPLEXES, ANTITUMOR, PALLADIUM(II), PD(II), LIGAND, DRUGS, RUTHENIUM(II), FLUORESCENCE
  • Karadeniz Technical University Affiliated: No


Four trans-palladium(II)- and trans-platinum(II)-chlorido complexes, trans-[PdCl2(2-hmpy)(2)] (1), trans-[PtCl2(2-hmpy)(2)] (2), trans-[Pdcl(2)(2-hepy)(2)] (3) and trans-[PtCl2(2-hepy)(2)] (4) (2-hmpy = 2-(hydroxymethyl)pyridine and 2-hepy = 2-(2-hydroxyethyl)pyridine), have been synthesized and characterized by elemental analysis, IR, NMR, and X-ray diffraction. The binding properties of these complexes with fish sperm DNA (FS-DNA) were investigated by UV titration, viscosity, thermal denaturation and electrophoresis measurements. The complexes can bind to FS-DNA and complex 4 exhibits the highest binding constant. Gel electrophoresis assay demonstrates that all the complexes can cleave the pCMV-beta gal plasmid DNA to a different degree. The cytotoxic activities of the complexes were tested against four different cancer cell lines. In general, the platinum(II) complexes are more effective than the isostructural palladium(II) complexes. Complex 4 shows high anticancer activity, compared to transplatin, cisplatin, carboplatin and oxaliplatin. (C) 2012 Elsevier Masson SAS. All rights reserved.