ACS Medicinal Chemistry Letters · 2019 · 78 citations · 16 references
MedicineMedicinal ChemistryOncologyCancer PharmacologyChemotherapyDrug DiscoveryOncology PharmacologyOvarian CancerAnticancer ActivityAnticancer ChemotherapyAnticancer Mechanism Of ActionAnticancer RepurposingMedicinal Chemistry ApplicationsOrthotopic Tumor ModelsOvarian Cancer ChemotherapyOvarian Cancer Treatment
In recent years, a few successful attempts were made to repurpose the clinically approved antiarthritic gold drug, Auranofin (AF), as an anticancer agent. The present study shows that the iodido(triethylphosphine)gold(I) complex, (Et3PAuI hereafter)—an AF analogue where the thiosugar ligand is simply replaced by one iodide ligand—manifests a solution chemistry resembling that of AF and exerts similar cytotoxic and proapoptotic effects on A2780 human ovarian cancer cells in vitro. However, when evaluated in a preclinical orthotopic model of ovarian cancer, Et3PAuI produces a far superior anticancer action than AF inducing a nearly complete tumor remission. The highly promising in vivo performances here documented for Et3PAuI warrant its further evaluation as a drug candidate for ovarian cancer treatment.
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