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dc.creatorRuberte, Ana Carolinaes_ES
dc.creatorRamos Inza, Sandraes_ES
dc.creatorAydillo, Carloses_ES
dc.creatorTalavera, Irenees_ES
dc.creatorEncío Martínez, Ignacioes_ES
dc.creatorPlano, Danieles_ES
dc.creatorSanmartín, Carmenes_ES
dc.date.accessioned2020-05-12T11:15:24Z
dc.date.available2020-05-12T11:15:24Z
dc.date.issued2020
dc.identifier.issn2076-3921
dc.identifier.urihttps://hdl.handle.net/2454/36864
dc.description.abstractSelenium compounds are pivotal in medicinal chemistry for their antitumoral and antioxidant properties. Forty seven acylselenoureas have been designed and synthesized following a fragment-based approach. Different scaffolds, including carbo-and hetero-cycles, along with mono-and bi-cyclic moieties, have been linked to the selenium containing skeleton. The dose-and time-dependent radical scavenging activity for all of the compounds were assessed using the in vitro 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) assays. Some of them showed a greater radical scavenging capacity at low doses and shorter times than ascorbic acid. Therefore, four compounds were evaluated to test their protective effects against H2O2-induced oxidative stress. One derivative protected cells against H2O2-induced damage, increasing cell survival by up to 3.6-fold. Additionally, in vitro cytotoxic activity of all compounds was screened against several cancer cells. Eight compounds were selected to determine their half maximal inhibitory concentration (IC50) values towards breast and lung cancer cells, along with their selectivity indexes. The breast cancer cells turned out to be much more sensitive than the lung. Two compounds (5d and 10a) stood out with IC50 values between 4.2 µM and 8.0 µM towards MCF-7 and T47D cells, with selectivity indexes greater than 22.9. In addition, compound 10b exhibited dual antioxidant and cytotoxic activities. Although further evidence is needed, the acylselenourea scaffold could be a feasible frame to develop new dual agents.en
dc.description.sponsorshipThis research was funded by PIUNA (refs 2014-26 and 2018-19), and C.S. and D.P. wish to express their gratitude to UNED-Pamplona, Fundación Bancaria 'La Caixa', and 'Fundación Caja Navarra' for financial support for the project.en
dc.format.extent16 p.
dc.format.mimetypeapplication/pdfen
dc.language.isoengen
dc.publisherMDPIen
dc.relation.ispartofAntioxidants, 2020, 9 (1), 55en
dc.rights© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) licenseen
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/
dc.subjectAcylselenoureasen
dc.subjectAntioxidanten
dc.subjectCytotoxicityen
dc.subjectOxidative stressen
dc.subjectRadical scavengingen
dc.subjectSeleniumen
dc.titleNovel N,N′-disubstituted acylselenoureas as potential antioxidant and cytotoxic agentsen
dc.typeinfo:eu-repo/semantics/articleen
dc.typeArtículo / Artikuluaes
dc.contributor.departmentUniversidad Pública de Navarra. Departamento de Ciencias de la Saludes_ES
dc.contributor.departmentNafarroako Unibertsitate Publikoa. Osasun Zientziak Sailaeu
dc.rights.accessRightsinfo:eu-repo/semantics/openAccessen
dc.rights.accessRightsAcceso abierto / Sarbide irekiaes
dc.identifier.doi10.3390/antiox9010055
dc.relation.publisherversionhttps://doi.org/10.3390/antiox9010055
dc.type.versioninfo:eu-repo/semantics/publishedVersionen
dc.type.versionVersión publicada / Argitaratu den bertsioaes


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© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access
article distributed under the terms and conditions of the Creative Commons Attribution
(CC BY) license
Except where otherwise noted, this item's license is described as © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license