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First generation of antioxidant precursors for bioisosteric Se-NSAIDs: design, synthesis, and in vitro and in vivo anticancer evaluation
dc.creator | Ramos Inza, Sandra | es_ES |
dc.creator | Aliaga, César | es_ES |
dc.creator | Encío Martínez, Ignacio | es_ES |
dc.creator | Raza, Asif | es_ES |
dc.creator | Sharma, Arun K. | es_ES |
dc.creator | Aydillo, Carlos | es_ES |
dc.creator | Martínez-Sáez, Nuria | es_ES |
dc.creator | Sanmartín, Carmen | es_ES |
dc.creator | Plano, Daniel | es_ES |
dc.date.accessioned | 2024-05-10T13:34:46Z | |
dc.date.available | 2024-05-10T13:34:46Z | |
dc.date.issued | 2023 | |
dc.identifier.citation | Ramos-Inza, S., Aliaga, C., Encío, I., Raza, A., Sharma, A. K., Aydillo, C., Martínez-Sáez, N., Sanmartín, C., Plano, D. (2023) First generation of antioxidant precursors for bioisosteric Se-NSAIDs: Design, synthesis, and in vitro and in vivo anticancer evaluation. Antioxidants, 12(9), 1-21. https://doi.org/10.3390/antiox12091666. | en |
dc.identifier.issn | 2076-3921 | |
dc.identifier.uri | https://hdl.handle.net/2454/48100 | |
dc.description.abstract | The introduction of selenium (Se) into organic scaffolds has been demonstrated to be a promising framework in the field of medicinal chemistry. A novel design of nonsteroidal anti-inflammatory drug (NSAID) derivatives based on a bioisosteric replacement via the incorporation of Se as diacyl diselenide is reported. The antioxidant activity was assessed using the DPPH radical scavenging assay. The new Se-NSAID derivatives bearing this unique combination showed antioxidant activity in a time- and dose-dependent manner, and also displayed different antiproliferative profiles in a panel of eight cancer cell lines as determined by the MTT assay. Ibuprofen derivative 5 was not only the most antioxidant agent, but also selectively induced toxicity in all the cancer cell lines tested (IC50 < 10 µM) while sparing nonmalignant cells, and induced apoptosis partially without enhancing the caspase 3/7 activity. Furthermore, NSAID derivative 5 significantly suppressed tumor growth in a subcutaneous colon cancer xenograft mouse model (10 mg/kg, TGI = 72%, and T/C = 38%) without exhibiting any apparent toxicity. To our knowledge, this work constitutes the first report on in vitro and in vivo anticancer activity of an unprecedented Se-NSAID hybrid derivative and its rational use for developing precursors for bioisosteric selenocompounds with appealing therapeutic applications. | en |
dc.description.sponsorship | This research was financially supported by the Plan de Investigación de la Universidad de Navarra, PIUNA (2018-19), and the Department of Pharmacology and Penn State Cancer Institute of the Penn State College of Medicine.; Sandra Ramos-Inza acknowledges the support of the FPU program from the Spanish Ministry of Universities for a Ph.D. fellowship (FPU18/04679) and a mobility grant (EST19/00898). | en |
dc.format.mimetype | application/pdf | en |
dc.language.iso | eng | en |
dc.publisher | MDPI | en |
dc.relation.ispartof | Antioxidants 2023, 12(9), 1666 | en |
dc.rights | © 2023 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. | en |
dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | |
dc.subject | Antioxidant | en |
dc.subject | Antiproliferative agents | en |
dc.subject | Colon cancer | en |
dc.subject | Diacyl diselenide | en |
dc.subject | Mouse xenograft model | en |
dc.subject | NSAID | en |
dc.subject | Selenium | en |
dc.title | First generation of antioxidant precursors for bioisosteric Se-NSAIDs: design, synthesis, and in vitro and in vivo anticancer evaluation | en |
dc.type | Artículo / Artikulua | es |
dc.type | info:eu-repo/semantics/article | en |
dc.date.updated | 2024-05-10T13:17:45Z | |
dc.contributor.department | Ciencias de la Salud | es_ES |
dc.contributor.department | Osasun Zientziak | eu |
dc.rights.accessRights | Acceso abierto / Sarbide irekia | es |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | en |
dc.identifier.doi | 10.3390/antiox12091666 | |
dc.relation.publisherversion | https://doi.org/10.3390/antiox12091666 | |
dc.type.version | Versión publicada / Argitaratu den bertsioa | es |
dc.type.version | info:eu-repo/semantics/publishedVersion | en |