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Synthesis, Chemical Characterization, and Biological Evaluation of Hydrophilic Gold(I) and Silver(I) N-Heterocyclic Carbenes as Potential Anticancer Agents.
Ceccherini, Valentina; Giorgi, Ester; Mannelli, Michele; Cirri, Damiano; Gamberi, Tania; Gabbiani, Chiara; Pratesi, Alessandro.
Afiliación
  • Ceccherini V; Department of Chemistry and Industrial Chemistry, University of Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy.
  • Giorgi E; Department of Chemistry and Industrial Chemistry, University of Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy.
  • Mannelli M; Department of Experimental and Clinical Biomedical Sciences "Mario Serio", University of Florence, Viale G.B. Morgagni 50, 50134 Firenze, Italy.
  • Cirri D; Department of Chemistry and Industrial Chemistry, University of Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy.
  • Gamberi T; Department of Experimental and Clinical Biomedical Sciences "Mario Serio", University of Florence, Viale G.B. Morgagni 50, 50134 Firenze, Italy.
  • Gabbiani C; Department of Chemistry and Industrial Chemistry, University of Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy.
  • Pratesi A; Department of Chemistry and Industrial Chemistry, University of Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy.
Inorg Chem ; 63(37): 16949-16963, 2024 Sep 16.
Article en En | MEDLINE | ID: mdl-39226133
ABSTRACT
A series of new gold(I) and silver(I) N-heterocyclic carbenes bearing a 1-thio-ß-d-glucose tetraacetate moiety was synthesized and chemically characterized. The compounds' stability and solubility in physiological conditions were investigated employing a multitechnique approach. Interaction studies with biologically relevant proteins, such as superoxide dismutase (SOD) and human serum albumin (HSA), were conducted via UV-vis absorption spectroscopy and high-resolution ESI mass spectrometry. The biological activity of the compounds was evaluated in the A2780 and A2780R (cisplatin-resistant) ovarian cancer cell lines and the HSkMC (human skeletal muscle) healthy cell line. Inhibition studies of the selenoenzyme thioredoxin reductase (TrxR) were also carried out. The results highlighted that the gold complexes are more stable in aqueous environment and capable of interaction with SOD and HSA. Moreover, these carbenes strongly inhibited the TrxR activity. In contrast, the silver ones underwent structural alterations in the aqueous medium and showed greater antiproliferative activity.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Plata / Reductasa de Tiorredoxina-Disulfuro / Ensayos de Selección de Medicamentos Antitumorales / Proliferación Celular / Oro / Compuestos Heterocíclicos / Metano / Antineoplásicos Límite: Humans Idioma: En Revista: Inorg Chem Año: 2024 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Plata / Reductasa de Tiorredoxina-Disulfuro / Ensayos de Selección de Medicamentos Antitumorales / Proliferación Celular / Oro / Compuestos Heterocíclicos / Metano / Antineoplásicos Límite: Humans Idioma: En Revista: Inorg Chem Año: 2024 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Estados Unidos