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

Natalia Estrada-Ortiz, Federica Guarra, Inge A. M. de Graaf, Lorella Marchetti, Marina H. de Jager, Geny M. M. Groothuis, Chiara Gabbiani, Angela Casini*

*Bijbehorende auteur voor dit werk

OnderzoeksoutputAcademicpeer review

31 Citaten (Scopus)
3 Downloads (Pure)

Samenvatting

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.

Originele taal-2English
Pagina's (van-tot)1429-1435
Aantal pagina's7
TijdschriftChemMedChem
Volume12
Nummer van het tijdschrift17
DOI's
StatusPublished - 7-sep-2017

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