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Repurposing antiplasmodial leads for cancer: Exploring the antiproliferative effects of N-cinnamoyl-aminoacridines

dc.contributor.authorFonte, Mélanie
dc.contributor.authorRôla, Catarina
dc.contributor.authorSantana, Sofia
dc.contributor.authorFerraz, Ricardo
dc.contributor.authorPrudêncio, Miguel
dc.contributor.authorAlmeida, Joana
dc.contributor.authorFerraz, Ricardo
dc.contributor.authorPrudêncio, Cristina
dc.contributor.authorTeixeira, Cátia
dc.contributor.authorGomes, Paula
dc.date.accessioned2024-10-09T10:09:43Z
dc.date.embargo2026-11
dc.date.issued2024-10
dc.description.abstractDrug repurposing and rescuing have been widely explored as cost-effective approaches to expand the portfolio of chemotherapeutic agents. Based on the reported antitumor properties of both trans-cinnamic acids and quinacrine, an antimalarial aminoacridine, we explored the antiproliferative properties of two series of N-cinnamoyl-aminoacridines recently identified as multi-stage antiplasmodial leads. The compounds were evaluated in vitro against three cancer cell lines (MKN-28, Huh-7, and HepG2), and human primary dermal fibroblasts. One of the series displayed highly selective antiproliferative activity in the micromolar range against the three cancer cell lines tested, without any toxicity to non-carcinogenic cells.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationFonte, M., Rôla, C., Santana, S., Prudêncio, M., Almeida, J., Ferraz, R., Prudêncio, C., Teixeira, C., & Gomes, P. (2024). Repurposing antiplasmodial leads for cancer: Exploring the antiproliferative effects of N-cinnamoyl-aminoacridines. Bioorganic & Medicinal Chemistry Letters, 111, 129894. https://doi.org/10.1016/j.bmcl.2024.129894pt_PT
dc.identifier.doi10.1016/j.bmcl.2024.129894pt_PT
dc.identifier.eissn1464-3405
dc.identifier.issn0960-894X
dc.identifier.urihttp://hdl.handle.net/10400.22/26225
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherElsevierpt_PT
dc.relationThe authors thank Professors Iva Fernandes (Food Quality and Technology group, Faculdade de Ciˆencias da Universidade do Porto, Portugal) and Pedro Coelho (T.Bio Laboratory, Escola Superior de Saúde do Polit´ecnico do Porto, Portugal), for the kind gift of MKN-28 and HDF cells, respectively. The authors further thank FCT/MCTES for supporting Research Units LAQV-REQUIMTE (LA/P/0008/2020 DOI 10.54499/ LA/P/0008/2020, UIDP/50006/2020 DOI 10.54499/UIDP/50006/ 2020 and UIDB/50006/2020 DOI 10.54499/UIDB/50006/2020) and for the Doctoral Grant to MF (SRFH/BD/147354/2019). MP further acknowledges the “la Caixa” Foundation for Grant HR21-848.pt_PT
dc.relation.publisherversionhttps://www.sciencedirect.com/science/article/pii/S0960894X24002968?via%3Dihubpt_PT
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/pt_PT
dc.subjectAntitumorpt_PT
dc.subjectCancerpt_PT
dc.subjectCovalent bitherapypt_PT
dc.subjectHybridpt_PT
dc.subjectMalariapt_PT
dc.subjectMepacrinept_PT
dc.subjectRecyclingpt_PT
dc.subjectSelectivitypt_PT
dc.titleRepurposing antiplasmodial leads for cancer: Exploring the antiproliferative effects of N-cinnamoyl-aminoacridinespt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.titleBioorganic & Medicinal Chemistry Letterspt_PT
oaire.citation.volume111pt_PT
person.familyNameALMEIDA
person.familyNameFerraz
person.familyNamePrudêncio
person.givenNameJOANA
person.givenNameRicardo
person.givenNameCristina
person.identifier1200571
person.identifier.ciencia-id1317-637D-8EE0
person.identifier.ciencia-id001E-71CE-F92D
person.identifier.ciencia-idC81E-F4EE-FADE
person.identifier.orcid0000-0001-8043-9053
person.identifier.orcid0000-0002-1761-117X
person.identifier.orcid0000-0002-9920-936X
person.identifier.ridG-5639-2011
person.identifier.scopus-author-id24464208500
person.identifier.scopus-author-id6508057930
rcaap.rightsembargoedAccesspt_PT
rcaap.typearticlept_PT
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relation.isAuthorOfPublication881a8ad5-ab13-4e49-89f4-08ca61cc81e3
relation.isAuthorOfPublication.latestForDiscoverya5a8faa7-12a5-4b1c-bced-44c895677397

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