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oai:riubu.ubu.es:10259/53402022-04-29T22:42:07Zcom_10259_4365com_10259_5086com_10259_2604col_10259_4366

Guarra, Federica Busto Vázquez, Natalia Guerri, Annalisa Marchetti, Lorella Marzo, Tiziano García Ruiz, Begoña Biver, Tarita 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. “la Caixa” Foundation (LCF/PR/PR12/11070003), Ministerio de Ciencia Innovación y Universidades-FEDER (RTI2018-102040-B-100) and Junta de Castilla y León-FEDER (BU305P18). application/pdf eng Elsevier Journal of Inorganic Biochemistry. 2020, V. 205, 110998 https://doi.org/10.1016/j.jinorgbio.2020.110998 info:eu-repo/grantAgreement/MICINN/RTI2018-102040-B-100 info:eu-repo/grantAgreement/JCyL/BU305P18 info:eu-repo/grantAgreement/FundaciónLaCaixa/LCF/PR/PR12/11070003 Attribution-NonCommercial-NoDerivatives 4.0 Internacional http://creativecommons.org/licenses/by-nc-nd/4.0/ info:eu-repo/semantics/openAccess Dual anticancer drug Metal carbene complexes Thioredoxin reductase Anthracenyl dyes DNA interactions Bioquímica Biochemistry Cytotoxic Ag(I) and Au(I) NHC-carbenes bind DNA and show TrxR inhibition info:eu-repo/semantics/article info:eu-repo/semantics/acceptedVersion Journal of Inorganic Biochemistry 205 110998