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.

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 / Tiziano Marzo, Lara Massai, Alessandro Pratesi, Matteo Stefanini, Damiano Cirri, Francesca Magherini, Matteo Becatti, Ida Landini, Stefania Nobili, Enrico Mini, Olivia Crociani, Annarosa Arcangeli, Serena Pillozzi, Tania Gamberi, Luigi Messori. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - STAMPA. - 10:4(2019), pp. 656-660. [10.1021/acsmedchemlett.9b00007]

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

Tiziano Marzo;Lara Massai;Alessandro Pratesi;Matteo Stefanini;Damiano Cirri;Francesca Magherini;Matteo Becatti;Ida Landini;Stefania Nobili;Enrico Mini;Olivia Crociani;Annarosa Arcangeli;Serena Pillozzi
;
Tania Gamberi;Luigi Messori
2019

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.
2019
10
656
660
Goal 3: Good health and well-being for people
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.
Tiziano Marzo, Lara Massai, Alessandro Pratesi, Matteo Stefanini, Damiano Cirri, Francesca Magherini, Matteo Becatti, Ida Landini, Stefania Nobili, En...espandi
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1152814
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