Ruthenium (II) nitrofurylsemicarbazone complexes: new DNA binding agents

Eur J Med Chem. 2004 Apr;39(4):377-82. doi: 10.1016/j.ejmech.2004.01.002.

Abstract

Complexes of the type [Ru(II)Cl(2)(DMSO)(2)L], where L are 5-nitrofurylsemicarbazone derivatives, were prepared in an effort to combine the potential anti-tumor activity of the metal and the free ligands. The new complexes are excellent DNA binding agents for calf thymus DNA. So, their in vitro anti-tumor activity was tested in cellular models and the complexes were found to be non-cytotoxic on the tumor cell lines assayed, neither in aerobic conditions nor in the bio-reductive assay performed. Redox behavior, lipophilicity and stability were studied in order to explain the lack of cellular cytotoxic effects. The complexes resulted 10-100 times more hydrophilic than the parent ligands thus the bio-activity of these compounds would be compromised by their inadequate lipophilic properties.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cattle
  • Cell Survival / drug effects
  • DNA / drug effects*
  • DNA / metabolism
  • DNA Adducts / chemistry
  • Drug Screening Assays, Antitumor
  • Nitroimidazoles / chemistry
  • Organometallic Compounds / chemistry
  • Organometallic Compounds / pharmacology
  • Oxidation-Reduction
  • Ruthenium / chemistry*
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • DNA Adducts
  • Nitroimidazoles
  • Organometallic Compounds
  • Ruthenium
  • DNA
  • calf thymus DNA