LAUSR

Abstract The last decade has witnessed tremendous advances in the design of anticancer gold complexes containing tertiary phosphines, a class of ligands that have significantly contributed to the development of metal complexes owing to their stabilizing effect. The promising in vitro antiproliferative properties of the phosphine-containing organogold compound auranofin [1-(thio-kS)-2,3,4,6-tetra-O-acetyl-β- d -glucopyranose](triethylphosphine-kP)gold(I), originally used to treat rheumatoid arthritis, inspired the extensive application of monodentate phosphines in the development of anticancer gold complexes. Meanwhile, the use of diphosphine ligands promoted advances in the preparation of chelated gold complexes as well as mixed-metal and mixed-ligand complexes that have superior anticancer activity. The present report summarizes the current state of knowledge of diphosphine ligands in the development of anticancer gold complexes, and explores challenges and opportunities in designing gold-containing mixed-metal and mixed-ligand complexes that have anticancer action.