Anticancer Organometallic Osmium(II)-p-cymene Complexes

ChemMedChem. 2015 Sep;10(9):1539-47. doi: 10.1002/cmdc.201500221. Epub 2015 Jul 14.

Abstract

Osmium compounds are attracting increasing attention as potential anticancer drugs. In this context, a series of bifunctional organometallic osmium(II)-p-cymene complexes functionalized with alkyl or perfluoroalkyl groups were prepared and screened for their antiproliferative activity. Three compounds from the series display selectivity toward cancer cells, with moderate cytotoxicity observed against human ovarian carcinoma (A2780) cells, whereas no cytotoxicity was observed on non-cancerous human embryonic kidney (HEK-293) cells and human endothelial (ECRF24) cells. Two of these three cancer-cell-selective compounds induce cell death largely via apoptosis and were also found to disrupt vascularization in the chicken embryo chorioallantoic membrane (CAM) model. Based on these promising properties, these compounds have potential clinical applications.

Keywords: antitumor agents; bioorganometallic chemistry; chorioallantoic membrane model; osmium complexes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Cell Line, Tumor / drug effects
  • Chemistry Techniques, Synthetic
  • Chick Embryo
  • Chorioallantoic Membrane / blood supply
  • Chorioallantoic Membrane / drug effects
  • Crystallography, X-Ray
  • Cymenes
  • Drug Screening Assays, Antitumor / methods
  • Endothelial Cells / drug effects
  • HEK293 Cells / drug effects
  • Humans
  • Monoterpenes / chemistry
  • Organometallic Compounds / chemistry*
  • Organometallic Compounds / pharmacology*
  • Osmium Compounds / chemistry
  • Osmium Compounds / pharmacology*
  • Ruthenium / chemistry

Substances

  • Antineoplastic Agents
  • Cymenes
  • Monoterpenes
  • Organometallic Compounds
  • Osmium Compounds
  • 4-cymene
  • Ruthenium