Antiproliferative activity of dmoPTA-Ru(II) complexes against human solid tumor cells

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4568-71. doi: 10.1016/j.bmcl.2011.05.116. Epub 2011 Jun 12.

Abstract

The biological evaluation of new Ru(II) complexes carrying dmoPTA (dmoPTA=3,7-dimethyl-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane) ligands is reported. The results on the biological activity revealed that the organometallic complexes are active against all cell lines with GI(50) values in the range 1.1-2.6 μM. When compared to the standard anticancer drug cisplatin, the bimetallic Ru(II) complexes showed a greater activity profile. The cell cycle analysis revealed that the new compounds induced arrest in G(1) phase. Contrary to cisplatin, these Ru(II) complexes do not interact with DNA. This result suggests that DNA might not be the key pharmacological target.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / therapeutic use
  • Antineoplastic Agents / toxicity
  • Cell Line, Tumor
  • Coordination Complexes / chemistry*
  • Coordination Complexes / therapeutic use
  • Coordination Complexes / toxicity
  • Drug Screening Assays, Antitumor
  • Humans
  • Neoplasms / drug therapy
  • Ruthenium / chemistry*

Substances

  • Antineoplastic Agents
  • Coordination Complexes
  • Ruthenium