Replacement of the Thiosugar of Auranofin with Iodide Enhances the Anticancer Potency in a Mouse Model of Ovarian Cancer

Abstract

In recent years, a few successful attempts were made to repurpose the clinically approved antiarthritic gold drug, Auranofin (<b>AF</b>), as an anticancer agent. The present study shows that the iodido(triethylphosphine)gold(I) complex, (<b>Et</b> _<b>3</b> <b>PAuI</b> hereafter)-an <b>AF</b> analogue where the thiosugar ligand is simply replaced by one iodide ligand-manifests a solution chemistry resembling that of <b>AF</b> and exerts similar cytotoxic and proapoptotic effects on A2780 human ovarian cancer cells <i>in vitro</i>. However, when evaluated in a preclinical orthotopic model of ovarian cancer, <b>Et</b> _<b>3</b> <b>PAuI</b> produces a far superior anticancer action than <b>AF</b> inducing a nearly complete tumor remission. The highly promising <i>in vivo</i> performances here documented for <b>Et</b> _<b>3</b> <b>PAuI</b> warrant its further evaluation as a drug candidate for ovarian cancer treatment.