2026-05-30T14:23:15Zhttps://riubu.ubu.es/oai/requestoai:riubu.ubu.es:10259/53402022-04-29T22:42:07Zcom_10259_4365com_10259_5086com_10259_2604col_10259_4366
Repositorio Institucional de la Universidad de Burgos
author
Guarra, Federica
author
Busto Vázquez, Natalia
author
Guerri, Annalisa
author
Marchetti, Lorella
author
Marzo, Tiziano
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García Ruiz, Begoña
author
Biver, Tarita
author
Gabbiani, Chiara
2020-06-10T12:29:12Z
2020-06-10T12:29:12Z
2020-04
0162-0134
http://hdl.handle.net/10259/5340
10.1016/j.jinorgbio.2020.110998
A silver(I) and a gold(I) complex of the fluorescent N-heterocyclic carbenic (NHC) ligand 1-(9-anthracenylmethyl)-3-(3-trimethylsilyl-2-propynil)-benzimidazol-2-ylidene have been synthesized and characterized. These compounds show cytotoxicity in the micromolar range and higher antiproliferative properties than cisplatin (CDDP) against several tumour cell lines such as SW480 (colon), A549 (lung) and HepG2 (liver). Both metal complexes are successfully internalized by SW480 cells being the silver compound the most accumulated. Subsequently, they were evaluated as inhibitors of the selenoenzyme Thioredoxin reductase (TrxR) and as DNA binders. Fluorescence microscopy confirmed that both protein and DNA binding could be involved in the biological activity of the compounds. The silver carbene was the most effective enzyme inhibitor with an IC50 in the nanomolar range. Also, interaction studies with natural double stranded DNA highlight a strong stabilisation of the double helix after binding to the Ag(I) carbene, indicating its potential suitability as dual-targeting anticancer active molecule.
eng
Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Dual anticancer drug
Metal carbene complexes
Thioredoxin reductase
Anthracenyl dyes
DNA interactions
Cytotoxic Ag(I) and Au(I) NHC-carbenes bind DNA and show TrxR inhibition
info:eu-repo/semantics/article
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