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Anticancer gold N-heterocyclic carbene complexes: a comparative in vitro and ex vivo study

Casini, Angela, Estrada-Ortiz, Natalia, Gabbiani, Chiara, Guarra, Federica, Groothuis, Geny, de Graaf, Inge, de Jager, Marina and Marchetti, Lorella 2017. Anticancer gold N-heterocyclic carbene complexes: a comparative in vitro and ex vivo study. ChemMedchem 12 (17) , pp. 1429-1435. 10.1002/cmdc.201700316

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Abstract

A series of organometallic Au(I) N-heterocyclic carbene (NHC) complexes was synthesized and characterized on 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 Au complexes ex vivo. All evaluated compounds presented cytotoxic activity towards the cancer cells in the nano- or low micromolar range. The mixed Au(I) NHC complex - (ter-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 towards the design of mixed NHC-alkynyl gold complexes for cancer therapy.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
Publisher: Wiley-Blackwell
ISSN: 1860-7179
Date of First Compliant Deposit: 9 August 2017
Date of Acceptance: 19 July 2017
Last Modified: 31 Aug 2018 15:22
URI: http://orca.cf.ac.uk/id/eprint/103453

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