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.
A simple synthetic entryway into (N-heterocyclic carbene)gold-steroidyl complexes and their anticancer activity
Scattolin T.;
2022
Abstract
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.File in questo prodotto:
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