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.
Replacement of the Thiosugar of Auranofin with Iodide Enhances the Anticancer Potency in a Mouse Model of Ovarian Cancer
Nobili S.;
2019-01-01
Abstract
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.File | Dimensione | Formato | |
---|---|---|---|
61 Marzo et al ACS Med Chem Lett 2019.pdf
Solo gestori archivio
Descrizione: Articolo principale
Tipologia:
PDF editoriale
Dimensione
1.91 MB
Formato
Adobe PDF
|
1.91 MB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.