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Anticancer Gold N-Heterocyclic Carbene Complexes: A Comparative in vitro and ex vivo Study

Estrada-Ortiz, N., Guarra, F., de Graaf, I. A. M., Marchetti, L., de Jager, M. H., Groothuis, G. M. M., Gabbiani, C. & Casini, A., 7-Sep-2017, In : ChemMedChem. 12, 17, p. 1429-1435 7 p.

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  • Anticancer Gold N-Heterocyclic Carbene Complexes:A Comparative in vitro and ex vivo Study

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DOI

A series of organometallic AuI N-heterocyclic carbene (NHC) complexes was synthesized and characterized for anticancer activity in four human cancer cell lines. The compounds' toxicity in healthy tissue was determined using precision-cut kidney slices (PCKS) as a tool to determine the potential selectivity of the gold complexes ex vivo. All evaluated compounds presented cytotoxic activity toward the cancer cells in the nano-or low micromolar range. The mixed AuI NHC complex, (tert-butylethynyl)-1,3-bis-(2,6-diisopropylphenyl) imidazol-2-ylidene gold(I), bearing an alkynyl moiety as ancillary ligand, showed high cytotoxicity in cancer cells in vitro, while being barely toxic in healthy rat kidney tissues. The obtained results open new perspectives toward the design of mixed NHC-alkynyl gold complexes for cancer therapy.

Original languageEnglish
Pages (from-to)1429-1435
Number of pages7
JournalChemMedChem
Volume12
Issue number17
Publication statusPublished - 7-Sep-2017

    Keywords

  • alkynyl compounds, cytotoxicity, gold NHC complexes, organometallics, precision-cut kidney slices, MEDICINAL INORGANIC-CHEMISTRY, BIOLOGICAL-PROPERTIES, GOLD(III) COMPLEXES, DNA-BINDING, AGENTS, CISPLATIN, PLATINUM, SLICES, CANCER, PALLADIUM(II)

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