A series of mono-, di-, and trinuclear organometallic alkynyl phosphane gold(I) complexes contg. the stable and water-sol. PTA and DAPTA ligands have been synthesized and characterized. The solid-state structure of one of these compds. was also established by x-ray crystallog. Luminescence was obsd. for most of these Au(I) alkynyl derivs. 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 compds. 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 compds. was detd. using epifluorescence microscopy. The presented results are discussed in relation to the putative mechanism of action of this family of gold-based cytotoxic agents.