In vitro anticancer activity evaluation of new cationic platinum(II) complexes based on imidazole moiety

Bioorg Med Chem. 2017 Mar 15;25(6):1907-1913. doi: 10.1016/j.bmc.2017.02.010. Epub 2017 Feb 14.

Abstract

The development and the synthesis of cationic platinum(II) complexes were realized and their cytotoxic activity was tested on triple negative breast cancer MDA-MB-231 cell line and in two cell lines poorly responsive to cisplatin (DLD-1 and MCF-7). The complex 2c resulted the most potent cytotoxic agent in MDA-MB-231 (IC50=61.9µM) and more effective than cisplatin on both DLD-1 (IC50=57.4µM) and MCF-7 (IC50=79.9µM) cell lines. 2c showed different cellular uptake and pharmacodynamic properties than cisplatin, interfering with the progression of the M phase of the cell cycle. Thus, 2c represents a lead compound of a new class of cytotoxic agents with promising antitumor activity.

Keywords: Cationic platinum complex; Cell cycle; Imidazole; Triple negative breast cancer; p53 expression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Division / drug effects
  • Cell Line, Tumor
  • Chromatography, High Pressure Liquid
  • Chromatography, Reverse-Phase
  • Drug Evaluation, Preclinical
  • Humans
  • Imidazoles / chemistry*
  • Organoplatinum Compounds / chemistry
  • Organoplatinum Compounds / pharmacology*
  • Triple Negative Breast Neoplasms / pathology*

Substances

  • Antineoplastic Agents
  • Imidazoles
  • Organoplatinum Compounds