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Oxidation of anticancer Pt(II) complexes with monodentate phosphane ligands: towards stable but active Pt(IV) prodrugs

Chem Commun (Camb). 2013 May 25;49(42):4806-8. doi: 10.1039/c3cc38416k.

Abstract

The synthesis, characterization and cytotoxicity studies of two novel platinum(IV) complexes, trans-PtCl4(dma)(PPh3), 1, and trans-PtCl4(ipa)(PPh3), 2, where dma is dimethylamine and ipa is isopropylamine, have been carried out. Both complexes contain aliphatic amines trans to phosphane ligands as a good alternative to take advantage of the phosphane group lipophilicity and the stability of platinum(IV) to obtain more effective drugs. Moreover, the complexes are stable in solution and such stability allowed their antitumoral action and DNA interaction to be checked and proved.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • DNA / metabolism
  • Glutathione / pharmacology
  • Humans
  • Ligands
  • Organoplatinum Compounds / chemistry*
  • Organoplatinum Compounds / pharmacology
  • Oxidation-Reduction
  • Phosphines / chemistry*
  • Prodrugs / chemistry*
  • Prodrugs / pharmacology

Substances

  • Antineoplastic Agents
  • Ligands
  • Organoplatinum Compounds
  • Phosphines
  • Prodrugs
  • DNA
  • Glutathione