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Replacement of the Thiosugar of Auranofin with Iodide Enhances the Anticancer Potency in a Mouse Model of Ovarian Cancer.
Marzo, Tiziano; Massai, Lara; Pratesi, Alessandro; Stefanini, Matteo; Cirri, Damiano; Magherini, Francesca; Becatti, Matteo; Landini, Ida; Nobili, Stefania; Mini, Enrico; Crociani, Olivia; Arcangeli, Annarosa; Pillozzi, Serena; Gamberi, Tania; Messori, Luigi.
Affiliation
  • Marzo T; Department of Pharmacy, University of Pisa, via Bonanno Pisano 6, 56126 Pisa, Italy.
  • Massai L; Laboratory of Metals in Medicine (MetMed), Department of Chemistry "U. Schiff", University of Florence, via della Lastruccia 3, 50019 Sesto Fiorentino, Italy.
  • Pratesi A; Laboratory of Metals in Medicine (MetMed), Department of Chemistry "U. Schiff", University of Florence, via della Lastruccia 3, 50019 Sesto Fiorentino, Italy.
  • Stefanini M; DI.V.A.L. Toscana s.r.l., via Madonna del Piano 6, 50019 Sesto Fiorentino, Italy.
  • Cirri D; Laboratory of Metals in Medicine (MetMed), Department of Chemistry "U. Schiff", University of Florence, via della Lastruccia 3, 50019 Sesto Fiorentino, Italy.
  • Magherini F; Department of Biochemical, Experimental and Clinical Sciences "Mario Serio", University of Florence, viale G.B. Morgagni 50, 50134 Firenze, Italy.
  • Becatti M; Department of Biochemical, Experimental and Clinical Sciences "Mario Serio", University of Florence, viale G.B. Morgagni 50, 50134 Firenze, Italy.
  • Landini I; Department of Health Sciences, University of Florence, viale Pieraccini 6, 50139 Firenze, Italy.
  • Nobili S; Department of Health Sciences, University of Florence, viale Pieraccini 6, 50139 Firenze, Italy.
  • Mini E; Department of Health Sciences, University of Florence, viale Pieraccini 6, 50139 Firenze, Italy.
  • Crociani O; DI.V.A.L. Toscana s.r.l., via Madonna del Piano 6, 50019 Sesto Fiorentino, Italy.
  • Arcangeli A; Department of Experimental and Clinical Medicine, University of Florence, viale G.B. Morgagni 50, 50134 Firenze, Italy.
  • Pillozzi S; DI.V.A.L. Toscana s.r.l., via Madonna del Piano 6, 50019 Sesto Fiorentino, Italy.
  • Gamberi T; Department of Experimental and Clinical Medicine, University of Florence, viale G.B. Morgagni 50, 50134 Firenze, Italy.
  • Messori L; Department of Biochemical, Experimental and Clinical Sciences "Mario Serio", University of Florence, viale G.B. Morgagni 50, 50134 Firenze, Italy.
ACS Med Chem Lett ; 10(4): 656-660, 2019 Apr 11.
Article in En | MEDLINE | ID: mdl-30996813
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, (Et 3 PAuI 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, Et 3 PAuI produces a far superior anticancer action than AF inducing a nearly complete tumor remission. The highly promising in vivo performances here documented for Et 3 PAuI warrant its further evaluation as a drug candidate for ovarian cancer treatment.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Language: En Journal: ACS Med Chem Lett Year: 2019 Type: Article Affiliation country: Italy
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Full text: 1 Collection: 01-internacional Database: MEDLINE Language: En Journal: ACS Med Chem Lett Year: 2019 Type: Article Affiliation country: Italy