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New Gold(I) organometallic compounds with biological activity in cancer cells

Bertrand, Benoit, de Almeida, Andreia, van der Burgt, Evelien P.M., Picquet, Michel, Citta, Anna, Folda, Alessandra, Rigobello, Maria Pia, Le Gendre, Pierre, Bodio, Ewen and Casini, Angela 2014. New Gold(I) organometallic compounds with biological activity in cancer cells. European Journal of Inorganic Chemistry 2014 (27) , pp. 4532-4536. 10.1002/ejic.201402248

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N-Heterocyclic carbene gold(I) complexes bearing a fluorescent coumarin ligand were synthesized and characterized by various techniques. The compounds were examined for their antiproliferative effects in normal and tumor cells in vitro; they demonstrated moderate activity and a certain degree of selectivity. The compounds were also shown to efficiently inhibit the selenoenzyme thioredoxin reductase (TrxR), whereas they were poorly effective towards the glutathione reductase (GR) and glutathione peroxidase enzymes. Notably, {3-[(7-methoxy-2-oxo-2H-chromen-4-yl)methyl]-1-methylimidazol-2-ylidene}(tetra-O-acetyl-1-thio-β-D-glucopyranosido)gold(I) (3) showed a pronounced inhibition of TrxR also in cell extracts, and it appeared to activate GR. Mechanistic information on the system derived from biotin-conjugated iodoacetamide assays showed selective metal binding to selenocysteine residues. Preliminary confocal fluorescence microscopy experiments proved that 3 enters tumor cells, where it reaches the nuclear compartment.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
Publisher: Wiley-Blackwell
ISSN: 1434-1948
Last Modified: 23 Jul 2020 01:43

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