Modulating the Anticancer Activity of Ruthenium(II)-Arene Complexes

J Med Chem. 2015 Apr 23;58(8):3356-65. doi: 10.1021/jm501655t. Epub 2015 Apr 7.

Abstract

Following the identification of [Ru(η(6)-p-cymene)Cl2(1H,1H,2H,2H-perfluorodecyl-3-(pyridin-3-yl)propanoate)], a ruthenium(II)-arene complex with a perfluoroalkyl-modified ligand that displays remarkable in vitro cancer cell selectivity, a series of structurally related compounds were designed. In the new derivatives, the p-cymene ring and/or the chloride ligands are substituted by other ligands to modulate the steric bulk or aquation kinetics. The new compounds were evaluated in both in vitro (cytotoxicity and migration assays) and in vivo (chicken chorioallantoic membrane) models and were found to exhibit potent antivascular effects.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / chemistry
  • Angiogenesis Inhibitors / pharmacology
  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Chick Embryo
  • Coordination Complexes / chemistry
  • Coordination Complexes / pharmacology
  • Crystallography, X-Ray
  • Cymenes
  • Humans
  • Models, Molecular
  • Monoterpenes / chemistry*
  • Monoterpenes / pharmacology*
  • Neoplasms / drug therapy
  • Ruthenium / chemistry*
  • Ruthenium / pharmacology*

Substances

  • Angiogenesis Inhibitors
  • Antineoplastic Agents
  • Coordination Complexes
  • Cymenes
  • Monoterpenes
  • 4-cymene
  • Ruthenium