ArticleAntioxidants (Basel, Switzerland)2026
Potent Nrf2-Inducing C6-Isothiocyanate Glucose Derivatives with Dual Antioxidant and Antitumor Activity.
Luis Alberto Prieto, Nora Khiar-Fernández, Rocío Calderón-Ruiz, Emelyne Giraud, José Manuel Calderón-Montaño, Jesús Lucia-Tamudo, Rafael León, José Antonio Pérez-Simón, Miguel López-Lázaro, Rocío Recio and 3 more
Abstract read
In one paragraphArticle in Antioxidants (Basel, Switzerland), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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What it found
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2 · The registryThe trial behind it
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4 · The recordCorrections and comments
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5 · Who and what moneyAuthors and funding
13 authors.
Luis Alberto PrietoDepartamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, 41012 Sevilla, Spain.ORCID 0000-0002-2172-6172 Nora Khiar-FernándezDepartamento de Química Orgánica I, Facultad de Ciencias Químicas, Universidad Complutense de Madrid, 28040 Madrid, Spain.ORCID 0000-0003-2195-5183 Rocío Calderón-RuizInstituto de Biomedicina de Sevilla (IBiS), Hospital Universitario Virgen del Rocío, Consejo Superior de Investigaciones Ccientíficas (CSIC), Universidad de Sevilla, 41013 Sevilla, Spain.ORCID 0000-0001-7311-9991 Emelyne GiraudDepartamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, 41012 Sevilla, Spain.ORCID 0009-0007-7673-9572 José Manuel Calderón-MontañoDepartamento de Farmacología, Facultad de Farmacia, Universidad de Sevilla, 41012 Sevilla, Spain.ORCID 0000-0001-6845-797X Jesús Lucia-TamudoFaculty of Chemistry and Pharmacy, Institute of Physical and Theoretical Chemistry, University of Regensburg, 93040 Regensburg, Germany.ORCID 0000-0002-1499-8225 Rafael LeónInstituto de Química Médica, Consejo Superior de Investigaciones Científicas (IQM-CSIC), 28006 Madrid, Spain.ORCID 0000-0003-4017-5756 José Antonio Pérez-SimónInstituto de Biomedicina de Sevilla (IBiS), Hospital Universitario Virgen del Rocío, Consejo Superior de Investigaciones Ccientíficas (CSIC), Universidad de Sevilla, 41013 Sevilla, Spain.ORCID 0000-0003-3616-6101 Miguel López-LázaroDepartamento de Farmacología, Facultad de Farmacia, Universidad de Sevilla, 41012 Sevilla, Spain.ORCID 0000-0003-2794-1647 Rocío RecioDepartamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, 41012 Sevilla, Spain.ORCID 0000-0002-7956-5295 Elena de la TorreInstituto de Biomedicina de Sevilla (IBiS), Hospital Universitario Virgen del Rocío, Consejo Superior de Investigaciones Ccientíficas (CSIC), Universidad de Sevilla, 41013 Sevilla, Spain.ORCID 0000-0003-2014-8013 Victoria ValdiviaDepartamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, 41012 Sevilla, Spain.ORCID 0000-0003-3534-7074 Inmaculada FernándezDepartamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, 41012 Sevilla, Spain.ORCID 0000-0002-3468-387X Funding
Ministerio de Ciencia, Innovación y Universidades PID2022-138863OB-I00Universidad de Sevilla VII PPIT-US
6 · The paper itselfAbstract
Isothiocyanates (ITCs) are well-known electrophilic agents with antioxidant and anticancer properties, largely attributed to their ability to activate the Nrf2/ARE pathway. Building on previous work with C1-ITC glycosyl derivatives, we designed and synthesized a new series of S-glycosyl isothiocyanates in which the ITC group was repositioned to the C6 carbon of the glucose scaffold. This structural rearrangement yielded stable and synthetically accessible derivatives with markedly enhanced biological profiles. Several compounds showed potent Nrf2 activation at non-cytotoxic concentrations, with CD values comparable to or exceeding those of natural ITCs. In parallel, the new C6-ITC derivatives displayed significant antiproliferative activity against leukemia and solid tumor cell lines. Among them, the phenylsulfone derivative
Indexed as
anticancer activityantileukemic activityIsothiocyanates (ITCs)Nrf2 activationS-glycosyl derivatives
Identifiers
PMID41596181
PMCPMC12837300
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