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

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 μM 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.