Synthesis, characterization and cytotoxicity of the gold(III) complexes of 4,5-dihydropyrazole-1-carbothioamide derivatives

Eur J Med Chem. 2011 May;46(5):1914-8. doi: 10.1016/j.ejmech.2011.02.031. Epub 2011 Feb 22.

Abstract

Eight new gold(III) complexes (1-8) of 5-aryl-3-(pyridin-2-yl)-4,5-dihydropyrazole-1-carbothioamide have been synthesized and characterized by elemental analysis, molar conductivity, IR, UV, 1H NMR, 13C NMR, MS, and thermal analysis techniques. The cytotoxicity was tested by MTT assay. The results indicate that the complexes 1-8 exert cytotoxic effects against HeLa and A549 cell lines. Moreover, the complexes 1, 4, 5, 7 and 8 have higher cytotoxicity than cisplatin against HeLa cell line. It suggests that the substituent groups on benzene have important effect on cytotoxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects
  • Drug Screening Assays, Antitumor
  • Gold / chemistry*
  • HeLa Cells
  • Humans
  • Ligands
  • Molecular Structure
  • Organogold Compounds / chemical synthesis
  • Organogold Compounds / chemistry
  • Organogold Compounds / pharmacology*
  • Pyrazoles / chemistry*
  • Stereoisomerism
  • Structure-Activity Relationship
  • Temperature
  • Thioamides / chemistry*
  • Tumor Cells, Cultured

Substances

  • 4,5-dihydropyrazole-1-carbothioamide
  • Antineoplastic Agents
  • Ligands
  • Organogold Compounds
  • Pyrazoles
  • Thioamides
  • Gold