Binuclear copper complexes: synthesis, X-ray structure and interaction study with nucleotide/protein by in vitro biochemical and electrochemical analysis

Eur J Med Chem. 2014 May 6:78:281-93. doi: 10.1016/j.ejmech.2014.03.043. Epub 2014 Mar 19.

Abstract

Two new, binuclear copper(II) hydrazone complexes have been synthesized and characterized by various physico-chemical techniques including single crystal X-ray diffraction. Interaction of these complexes with nucleotide and protein were analyzed by in vitro biochemical and electrochemical analysis. Both the complexes exhibited intercalative mode of binding with DNA. Further, gel electrophoresis assay demonstrated the ability of the complexes to cleave the supercoiled pBR322 plasmid DNA to nicked circular DNA form. Cytotoxicity of the complexes performed against a panel of cancer cell lines and a normal cell line proved that these complexes are potentially cytotoxic against the cancerous cell lines, particularly with IC50 as low as 0.7 μM against HeLa cell line.

Keywords: Binuclear copper complex; Cytotoxicity; Nucleotide and protein interaction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cattle
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Copper / chemistry*
  • Crystallography, X-Ray
  • DNA / chemistry
  • DNA / drug effects*
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Electrochemical Techniques*
  • HeLa Cells
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Organometallic Compounds / chemical synthesis
  • Organometallic Compounds / chemistry
  • Organometallic Compounds / pharmacology*
  • Serum Albumin / chemistry*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Organometallic Compounds
  • Serum Albumin
  • Copper
  • DNA