Phosphine-bridged dinuclear gold(I) alkynyl complexes: Thioredoxin reductase inhibition and cytotoxicity

The study of the biological properties of four dinuclear gold(I) alkynyl complexes with general formulae [(μ2-diphos)(AuCCC5H4N)2] (diphos = dcypm, dcypb, dppm and dppb) is reported in this work. The biological evaluation included enzymatic inhibition and tumor cell proliferation studies. Inhibition of the enzyme thioredoxin reductase (TrxR) was confirmed for the gold derivatives containing dppm and dppb bridging ligands and indicated a preference for the shorter bridging ligand. Strong cytotoxic activities against two different cultured tumor cell lines (MCF-7 and HT-29) were noted for most of the compounds but were not correlated with an activity against TrxR.

The synthesis, characterization and biological activity of a series of bridged dinuclear gold(I) alkynyl complexes is reported. They present a good potential for developing biologically active gold(I) complexes.Figure optionsDownload as PowerPoint slideHighlights
► The biological properties of four dinuclear gold(I) alkynyl complexes is studied.
► Enzymatic inhibition and tumor cell proliferation studies are carried out.
► Strong cytotoxic activities against MCF-7 and HT-29 cultured tumor cell lines.
► Well-resolved emission bands are observed between 400 and 575 nm in DMSO.