Novel phosphine sulphide gold(i) complexes: topoisomerase I inhibitors and antiproliferative agents.

This work describes the synthesis of gold(I) complexes of phosphine sulphides. The formation of these new derivatives has been confirmed by X-ray crystallography. The coordination of gold(I) with the sulphur atom of phosphine sulphides favors the inhibition of topoisomerase I, as well as a high cytotoxicity of the gold(I) complexed compounds against cancer line A549 with IC50 values in the nanomolar range and with IC50 values below 5 microM against the SKOV3 cell line. It should be noted that the cytotoxicities observed for the new gold(I) complexes are higher than those observed for phosphine sulphide ligands before binding to gold. Furthermore, the results presented also indicate that the presence of a nitrogenated heterocycle, such as tetrahydroquinoline or quinoline, is also necessary for the TopI inhibition to be maintained. In addition, no toxicity was observed when the non-cancerous lung fibroblast cell line (MRC5) was treated with the new phosphine sulphide gold(I) complexes prepared.