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Novel phosphine sulphide gold(I) complexes: topoisomerase I inhibitors and antiproliferative agents
dc.contributor.author | Martín Encinas, Endika | |
dc.contributor.author | Cornejo Rodríguez, Verónica | |
dc.contributor.author | Miguel, Jesús Ángel | |
dc.contributor.author | Martinez-Ilarduya, Jesus M. | |
dc.contributor.author | Rubiales Alcaine, María Gloria | |
dc.contributor.author | Knudsen, Birgitta R. | |
dc.contributor.author | Palacios Gambra, Francisco Javier | |
dc.contributor.author | Alonso Pérez, Concepción Estibaliz | |
dc.date.accessioned | 2024-04-10T15:38:11Z | |
dc.date.available | 2024-04-10T15:38:11Z | |
dc.date.issued | 2020-05-20 | |
dc.identifier.citation | Dalton Transactions 49(23) : 7852-7861 (2020) | es_ES |
dc.identifier.issn | 1477-9226 | |
dc.identifier.issn | 1477-9234 | |
dc.identifier.uri | http://hdl.handle.net/10810/66604 | |
dc.description.abstract | This work describes the synthesis of the gold(I) complexes of phosphine sulphides. The formation of these new derivatives has been confirmed by X-ray crystallography. The coordination of gold(I) with the sulphur atom of the phosphine sulphides favors the inhibition of topoisomerase I as well as a high cytotoxicity of the gold(I)-complexed compounds against the cancer line A549 with IC50 values in the nanomolar range and IC50 values below 5 μM against the SKOV3 cell line. It should be noted that the cytotoxicities observed for the new gold(I) complexes are higher than those observed for phosphine sulphide ligands before binding to gold. Furthermore, the results also indicate that the presence of a nitrogenated heterocycle, such as tetrahydroquinoline or quinoline, is also necessary for the TopI inhibition to be maintained. In addition, no toxicity was observed when the non-cancerous lung fibroblast cell line (MRC5) was treated with the new phosphine sulphide gold(I) complexes prepared. | es_ES |
dc.description.sponsorship | Financial support from the Ministerio de Ciencia, Innovación y Universidades (MCIU), Agencia Estatal de Investigación (AEI) y Fondo Europeo de Desarrollo Regional (FEDER; RTI2018-101818-B-I00, UE), Ministerio de Economía y Empresa (MINECO, CTQ2017-89217P) and by Gobierno Vasco, Universidad del País Vasco (GV, IT 992-16; UPV) is gratefully acknowledged. Technical and human support provided by IZO-SGI, SGIker (UPV/EHU, MICINN, GV/EJ, ERDF and ESF) are gratefully acknowledged. | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | RSC | es_ES |
dc.relation | info:eu-repo/grantAgreement/MCIU/RTI2018-101818-B-I00 | es_ES |
dc.rights | info:eu-repo/semantics/openAccess | es_ES |
dc.title | Novel phosphine sulphide gold(I) complexes: topoisomerase I inhibitors and antiproliferative agents | es_ES |
dc.type | info:eu-repo/semantics/article | es_ES |
dc.rights.holder | © 2020 The Royal Society of Chemistry | es_ES |
dc.relation.publisherversion | https://pubs.rsc.org/en/content/articlelanding/2020/dt/d0dt01467b | es_ES |
dc.relation.publisherversion | info:eu-repo/grantAgreement/MINECO/CTQ2017-89217P | es_ES |
dc.identifier.doi | 10.1039/D0DT01467B | |
dc.departamentoes | Química orgánica I | es_ES |
dc.departamentoeu | Kimika organikoa I | es_ES |