A straightforward procedure to gold-steroidyl complexes bearing saturated and unsaturated NHC ligands is reported. These derivatives display good cytotoxicity against a panel of cancer cell lines with IC₅₀ values in the low micromolar range. Cellular uptake of the most active complex into MCF-7 breast cancer cells was facilitated by the coordinated ethisterone ligand.

A straightforward synthetic route to new N-heterocyclic carbene (NHC)-gold-steroidyl complexes is reported. The desired complexes were obtained using a weak base (such as K₂CO₃) through a concerted-metallation-deprotonation (CMD) reaction mechanism occurring between [Au(NHC)Cl] and ethisterone as a model steroid-based alkyne. Most complexes displayed good cytotoxicity against a panel of cancer cell lines with IC₅₀ values in the low micromolar range. Cellular uptake of the most active complex 2a into MCF-7 breast cancer cells was facilitated by the coordinated ethisterone ligand.