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In vitro and in vivo evaluation of novel chromeno[2,3-d]pyrimidinones as therapeutic agents for triple negative breast cancer

2024-02-20Research article Open access
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dc.contributor.authorCarvalho, Luísa
dc.contributor.authorLima, Fábio Pedroso de
dc.contributor.authorCerqueira, Mónica
dc.contributor.authorSilva, Ana
dc.contributor.authorPontes, Olívia
dc.contributor.authorOliveira-Pinto, Sofia
dc.contributor.authorGuerreiro, Sara
dc.contributor.authorCosta, Marta D.
dc.contributor.authorGranja, Sara
dc.contributor.authorMaciel, Patrícia
dc.contributor.authorLongatto-Filho, Adhemar
dc.contributor.authorBaltazar, Fátima
dc.contributor.authorProença, Fernanda
dc.contributor.authorCosta, Marta
dc.contributor.authorGranja, Sara
dc.date.accessioned2025-06-18T08:41:36Z
dc.date.available2025-06-18T08:41:36Z
dc.date.issued2024-02-20
dc.description.abstractTriple-negative breast cancer (TNBC) is the most aggressive subtype of breast cancer, and the limited therapeutic options show poor efficacy in patients, associated to severe side effects and development of resistance. Considering that chromene-based scaffolds proved to be attractive candidates for cancer therapy, herein we prepared new chromeno[2,3-d]pyrimidinone derivatives by a simple two step procedure, starting from the reaction of cyanoacetamide and a salicylaldehyde. A cell viability screening in several breast cancer cell lines allowed to identify two promising compounds with IC50 values in the low micromolar range for TNBC cells. These chromenes inhibited cell proliferation, induced cell cycle arrest and triggered cell death through apoptosis. In vivo studies revealed a safe profile in invertebrate and vertebrate animal models and confirmed their capacity to inhibit tumor growth in the CAM model, inducing significant tumor regression after 4 days of treatment. The two compounds identified in this study are promising drug candidates for TNBC treatment and valuable hits for future optimization, using the versatile synthetic platform that was developed.por
dc.description.sponsorshipREDE/1517/RMN/2005
dc.identifier.citationCarvalho, L., Lima, F. P. de, Cerqueira, M., Silva, A., Pontes, O., Oliveira-Pinto, S., Guerreiro, S., Costa, M. D., Granja, S., Maciel, P., Longatto-Filho, A., Baltazar, F., Proença, F., & Costa, M. (2024). In vitro and in vivo evaluation of novel chromeno[2,3-d]pyrimidinones as therapeutic agents for triple negative breast cancer. RSC Medicinal Chemistry, 15(4), 1362–1380. https://doi.org/10.1039/D3MD00682D
dc.identifier.doi10.1039/D3MD00682D
dc.identifier.urihttp://hdl.handle.net/10400.22/30156
dc.language.isoeng
dc.peerreviewedyes
dc.publisherRoyal Society of Chemistry
dc.relationproject UIDB/ 50026/2020 and UIDP/50026/2020; project NORTE- 01-0145-FEDER-000055
dc.relation.hasversionhttps://pmc.ncbi.nlm.nih.gov/articles/PMC11042168/pdf/MD-015-D3MD00682D.pdf
dc.rights.uriN/A
dc.subjectChromeno[2
dc.subject3-d]pyrimidinones
dc.subjectBreast cancer
dc.titleIn vitro and in vivo evaluation of novel chromeno[2,3-d]pyrimidinones as therapeutic agents for triple negative breast cancerpor
dc.typeresearch article
dspace.entity.typePublication
oaire.citation.endPage1380
oaire.citation.startPage1362
oaire.citation.titleRSC Medical Chemistry
oaire.citation.volume15
oaire.versionhttp://purl.org/coar/version/c_970fb48d4fbd8a85
person.familyNameGranja
person.givenNameSara
person.identifier.ciencia-idC41F-02E4-065E
person.identifier.orcid0000-0001-8717-6751
relation.isAuthorOfPublication06306a95-9c06-47c7-b2e5-5bbf757bec17
relation.isAuthorOfPublication.latestForDiscovery06306a95-9c06-47c7-b2e5-5bbf757bec17

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