Platinum(II) complexes with mono-aminophosphonate ester targeting group that induce apoptosis through G1 cell-cycle arrest: synthesis, crystal structure and antitumour activity

Eur J Med Chem. 2013 May:63:76-84. doi: 10.1016/j.ejmech.2013.01.055. Epub 2013 Feb 9.

Abstract

Six new platinum(II) complexes with mono-aminophosphonate ester were synthesized and characterized by elemental analysis, (1)H NMR, ESI-MS as well as single crystal X-ray diffraction analysis. They are mononuclear structures. In all the crystal structures of complexes 1-6, the platinum centre adopts an approximately square-planar geometry, which were found to possess excellent solubility in both organic solvents and water and exhibit considerable cytotoxicity against MG-63, SK-OV-3 and HepG2 cell lines, but low cytotoxicity towards normal human liver cell HL-7702. In contrast to cisplatin, their antitumour activities are achieved through the induction of cell apoptosis by G1 cell-cycle arrest.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects*
  • Cell Line
  • Cell Line, Tumor
  • Crystallography, X-Ray
  • Drug Screening Assays, Antitumor
  • Flow Cytometry
  • G1 Phase Cell Cycle Checkpoints / drug effects*
  • Hep G2 Cells
  • Humans
  • Models, Chemical
  • Molecular Structure
  • Organophosphonates / chemistry*
  • Organoplatinum Compounds / chemical synthesis
  • Organoplatinum Compounds / chemistry
  • Organoplatinum Compounds / pharmacology*
  • Platinum / chemistry*
  • Structure-Activity Relationship

Substances

  • Organophosphonates
  • Organoplatinum Compounds
  • Platinum