Antiproliferative Activity of Gold(I) Alkyne Complexes Containing Water-Soluble Phosphane Ligands

Elena Vergara, Elena Cerrada, Angela Casini, Olivier Zava, Mariano Laguna*, Paul J. Dyson

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

91 Citations (Scopus)

Abstract

A series of mono-, di-, and trinuclear organometallic alkynyl phosphane gold(I) complexes containing the stable and water-soluble PTA and DAPTA ligands have been synthesized and characterized. The solid-state structure of one of these compounds was also established by X-ray crystallography. Luminiscence was observed for most of these Au(I) alkynyl derivatives in the solid state. The cytotoxicity of the complexes was evaluated on A2780 ovarian cancer cells and on their cisplatin-resistant cell line A2780cisR; the compounds showed an activity in the low mu M range, being markedly more active than cisplatin in the A2780cisR cell line. The intracellular distribution of some representative compounds was determined using epifluorescence microscopy. The presented results are discussed in relation to the putative mechanism of action of this family of gold-based cytotoxic agents.

Original languageEnglish
Pages (from-to)2596-2603
Number of pages8
JournalOrganometallics
Volume29
Issue number11
DOIs
Publication statusPublished - 14-Jun-2010
Externally publishedYes

Keywords

  • IN-VITRO CYTOTOXICITY
  • HETEROCYCLIC CARBENE COMPLEXES
  • BOVINE SERUM-ALBUMIN
  • PHOTOLUMINESCENT PROPERTIES
  • COORDINATION-COMPLEXES
  • THIOREDOXIN REDUCTASE
  • RATIONAL DESIGN
  • CANCER-CELLS
  • 1,3,5-TRIAZA-7-PHOSPHAADAMANTANE
  • INHIBITION

Cite this