Thermal characterization, polymorphism, and stability evaluation of Se-NSAID derivatives with potent anticancer activity

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dc.contributor.authorRamos Inza, Sandra
dc.contributor.authorAlmagro, Eneko
dc.contributor.authorFont, María
dc.contributor.authorEncío Martínez, Ignacio
dc.contributor.authorPlano, Daniel
dc.contributor.authorSanmartín, Carmen
dc.contributor.authorSirera, Rafael
dc.contributor.authorLizarraga, Elena
dc.contributor.departmentCiencias de la Saludes_ES
dc.contributor.departmentOsasun Zientziakeu
dc.date.accessioned2024-05-16T18:30:40Z
dc.date.available2024-05-16T18:30:40Z
dc.date.issued2024
dc.date.updated2024-05-16T18:04:16Z
dc.description.abstractStability, thermal characterization, and identification of possible polymorphism are relevant in the development of novel therapeutic drugs. In this context, thirty new nonsteroidal anti-inflammatory drug (NSAID) derivatives containing selenium (Se) as selenoesters or diacyl diselenides with demonstrated anticancer activity were thermally characterized in order to establish thermal stability criteria and detect possible polymorphic forms. Compounds were analyzed by a combination of thermogravimetry, differential scanning calorimetry, and X-ray diffraction techniques, and five different calorimetric behaviors were identified. Two compounds based on naproxen (I.3d and I.3e) and an indomethacin-containing derivative (II.2) presented two crystalline forms. The stability under acid, alkaline and oxidative conditions of selected polymorphs was also assessed using high-performance liquid chromatography. In addition, the cytotoxic activity of Se-NSAID crystalline polymorphs was studied in several cancer cell lines in vitro. Remarkably, no significant differences were found among the polymorphic forms tested, thus proving that these compounds are thermally qualified for further drug development.en
dc.description.sponsorshipThis work was financially supported by the Plan de Investigación de la Universidad de Navarra, PIUNA (2018-19), and the department of Pharmaceutical Technology and Chemistry of the University of Navarra. Partial financial support was received from the department of Chemistry of the University of Navarra. Sandra Ramos Inza wishes to express her gratitude to the FPU program from the Spanish Ministry of Universities for a Ph.D. grant (FPU18/04679). Open Access funding provided thanks to the CRUE-CSIC agreement with Springer Nature.en
dc.format.mimetypeapplication/pdfen
dc.format.mimetypeapplication/msworden
dc.identifier.citationRamos-Inza, S., Almagro, E., Font, M., Encío, I., Plano, D., Sanmartín, C., Sirera, R., Lizarraga, E. (2024) Thermal characterization, polymorphism, and stability evaluation of Se-NSAID derivatives with potent anticancer activity. Journal of Thermal Analysis and Calorimetry, 149, 1015-1028. https://doi.org/10.1007/s10973-023-12756-3.en
dc.identifier.doi10.1007/s10973-023-12756-3
dc.identifier.issn1388-6150
dc.identifier.urihttps://academica-e.unavarra.es/handle/2454/48119
dc.language.isoengen
dc.publisherSpringeren
dc.relation.ispartofJournal of Thermal Analysis and Calorimetry (2024), 149, 1015-1028en
dc.relation.publisherversionhttps://doi.org/10.1007/s10973-023-12756-3
dc.rights© The Author(s) 2023. This article is licensed under a Creative Commons Attribution 4.0 International License.en
dc.rights.accessRightsinfo:eu-repo/semantics/openAccess
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.subjectCytotoxicityen
dc.subjectNSAIDen
dc.subjectPolymorphismen
dc.subjectSeleniumen
dc.subjectTG/DSC analysisen
dc.subjectX-ray diffractionen
dc.titleThermal characterization, polymorphism, and stability evaluation of Se-NSAID derivatives with potent anticancer activityen
dc.typeinfo:eu-repo/semantics/article
dc.type.versioninfo:eu-repo/semantics/publishedVersion
dspace.entity.typePublication
relation.isAuthorOfPublication599ca381-1fd2-4a23-93ab-4373837eb6e0
relation.isAuthorOfPublication.latestForDiscovery599ca381-1fd2-4a23-93ab-4373837eb6e0

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