Anti-tumor activities of Au(I) complexed with bisphosphines in HL-60 cells

J Inorg Biochem. 2014 Aug:137:109-14. doi: 10.1016/j.jinorgbio.2014.04.006. Epub 2014 Apr 22.

Abstract

We found that Au(I) complexed with 2,3-bis(tert-butyl(methyl)phosphino) quinoxaline (10) was a potent anti-tumor agent (half-maximal growth inhibitory concentration, GI50=0.87μM) with broad anti-tumor activity. In particular, the activity of complex 10 was high in tumor cell lines derived from the colon and ovary. Treatment with complex 10 resulted in the apoptosis of HL-60 cells. The ligand for the preparation of complex 10 is commercially available implying that complex 10 might be a good drug candidate for cancer therapy.

Keywords: 2,3-bis(tert-butyl(methyl)phosphino) quinoxaline; Anti-tumor activity; Au(I) complex.

MeSH terms

  • Apoptosis / drug effects
  • Carbamates / administration & dosage
  • Carbamates / chemistry*
  • Cell Proliferation / drug effects*
  • Colonic Neoplasms / drug therapy
  • Colonic Neoplasms / pathology
  • Drug Screening Assays, Antitumor
  • Female
  • Gold / administration & dosage
  • Gold / chemistry*
  • HL-60 Cells
  • Humans
  • Ovarian Neoplasms / chemically induced
  • Ovarian Neoplasms / drug therapy
  • Pyrrolizidine Alkaloids / administration & dosage
  • Pyrrolizidine Alkaloids / chemistry*

Substances

  • Carbamates
  • Pyrrolizidine Alkaloids
  • synthanecine A-bis(N-ethylcarbamate)
  • Gold