Diamminetetrakis(carboxylato)platinum(IV) complexes--synthesis, characterization, and cytotoxicity

Chem Biodivers. 2012 Sep;9(9):1840-8. doi: 10.1002/cbdv.201200019.

Abstract

A series of eight novel diamminetetrakis(carboxylato)platinum(IV) complexes was synthesized and characterized by multinuclear (1)H-, (13)C-, (15)N-, and (195)Pt-NMR spectroscopy. Their antiproliferative potency was evaluated in three human cancer cell lines representing ovarian (CH1), lung (A549), and colon carcinoma (SW480). In cisplatin-sensitive CH1 cancer cells, cytotoxicity was found in the low micromolar range, whereas, in inherently cisplatin-resistant A549 and SW480 cells, the activity was very low or negligible. Astonishingly, raise in lipophilicity of the complexes, as found in the case of cisplatin analogs, did not result in a significant enhancement of the cytotoxic effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / toxicity
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cisplatin / chemistry*
  • Cisplatin / pharmacology
  • Drug Screening Assays, Antitumor
  • Humans
  • Inhibitory Concentration 50
  • Magnetic Resonance Spectroscopy
  • Neoplasms
  • Organoplatinum Compounds / chemical synthesis*
  • Organoplatinum Compounds / chemistry
  • Organoplatinum Compounds / toxicity

Substances

  • Antineoplastic Agents
  • Organoplatinum Compounds
  • Cisplatin