New melatonin–cinnamate hybrids as multi-target drugs for neurodegenerative diseases: Nrf2-induction, antioxidant effect and neuroprotection

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dc.contributor.authorBuendia, Izaskun
dc.contributor.authorNavarro González De Mesa, Elisa
dc.contributor.authorMichalska Dziama, Patrycja
dc.contributor.authorGameiro, Isabel
dc.contributor.authorEgea, Javier
dc.contributor.authorAbril, Sheila
dc.contributor.authorLópez, Alicia
dc.contributor.authorGonzález-Lafuente, Laura
dc.contributor.authorG. López, Manuela
dc.contributor.authorLeón Martínez, Rafael
dc.date.accessioned2024-01-31T12:20:07Z
dc.date.available2024-01-31T12:20:07Z
dc.date.issued2015-10-23
dc.description.abstractNeurodegenerative diseases share many pathological pathways, such as abnormal protein aggregation, mitochondrial dysfunction, extensive oxidative stress and neuroinflammation. Cells have an intrinsic mechanism of protection, the Nrf2 transcriptional factor, known as the master regulator of redox homeostasis. Results: Based on the common features of these diseases we have designed a multi-target hybrid structure derived from melatonin and ethyl cinnamate. The obtained derivatives were Nrf2 inducers and potent-free radical scavengers. These new compounds showed a very interesting neuroprotective profile in several in vitro models of oxidative stress, Alzheimer's disease and brain ischemia. Conclusion: We have designed a new hybrid structure with complementary activities. We have identified compound 5h as an interesting Nrf2 inducer, very potent antioxidant and neuroprotectant.
dc.description.departmentDepto. de Química en Ciencias Farmacéuticas
dc.description.facultyFac. de Farmacia
dc.description.refereedTRUE
dc.description.sponsorshipEuropean Commission
dc.description.sponsorshipMinisterio de Sanidad(España)
dc.description.sponsorshipMinisterio de Economía, Comercio y Empresa(España)
dc.description.sponsorshipInstituto de Salud Carlos III
dc.description.sponsorshipMinisterio de Educación, Cultura y Deporte(España)
dc.description.statuspub
dc.identifier.doi10.4155/fmc.15.99
dc.identifier.essn1756-8927
dc.identifier.issn1756-8919
dc.identifier.officialurlhttps://doi.org/10.4155/fmc.15.99
dc.identifier.urihttps://hdl.handle.net/20.500.14352/97103
dc.issue.number15
dc.journal.titleFuture Medicinal Chemistry
dc.language.isoeng
dc.relation.projectIDinfo:eu-repo/grantAgreement/PCIG11-GA-2012-322156
dc.relation.projectIDinfo:eu-repo/grantAgreement/CP14/00008
dc.relation.projectIDinfo:eu-repo/grantAgreement/AP2010-1219
dc.relation.projectIDinfo:eu-repo/grantAgreement/FPU13/03737
dc.relation.projectIDinfo:eu-repo/grantAgreement/MINECO/SAF2012-32223
dc.rights.accessRightsrestricted access
dc.subject.cdu615.01/.03
dc.subject.keywordOxidative stress
dc.subject.keywordNrf2 inducer
dc.subject.keywordMelatonin
dc.subject.ucmFarmacología (Farmacia)
dc.subject.unesco3209.99 Otras
dc.titleNew melatonin–cinnamate hybrids as multi-target drugs for neurodegenerative diseases: Nrf2-induction, antioxidant effect and neuroprotection
dc.typejournal article
dc.type.hasVersionVoR
dc.volume.number7
dspace.entity.typePublication
relation.isAuthorOfPublicationd0e22d4d-2011-4a9f-bd9c-609855dba391
relation.isAuthorOfPublication298927e3-bd5b-46ad-bdbe-b818ade8cfb1
relation.isAuthorOfPublication7093c6ce-e368-44f0-a993-8f7212cb1c2a
relation.isAuthorOfPublication.latestForDiscoveryd0e22d4d-2011-4a9f-bd9c-609855dba391
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