Biological evaluation of donor-acceptor aminonaphthoquinones as antitumor agents

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dc.contributor.authorBenites, Julio
dc.contributor.authorValderrama, Jaime A.
dc.contributor.authorBettega, Karina
dc.contributor.authorPedrosa, Rozangela Curi
dc.contributor.authorBuc Calderon, Pedro
dc.contributor.authorVerrax, Julien
dc.date.accessioned2024-01-10T12:04:28Z
dc.date.available2024-01-10T12:04:28Z
dc.date.issued2010
dc.description.abstractSeveral members of the phenylamino-1,4-naphthoquinone series were prepared in order to investigate structure-activity relationships (SAR) and to explore the antitumor effects associated with this scaffold. The cytotoxic effects of the aminoquinones (EC50) against a panel of cancer cell lines (MCF7, DU145 and T24 cells) and healthy fibroblasts (BALB/3T3) were assessed in vitro using the MTT reduction assay 48 h after drug exposure. SAR analysis of the aminonaphthoquinone series showed that insertion of a chlorine atom in the acceptor quinone nucleus and/or insertion of a methyl group at the nitrogen atom of the donor phenylamino group induced significant changes in cytotoxic activity. Quinones 7 and 9, which exhibited the highest selective indexes (5.73 and 6.29, respectively), were further characterized using the following assays: Colony formation, caspase-3 activity, and ATP content. The results showed that aminoquinone 7 strongly influenced ATP levels and impaired the proliferative capacity of T24 cells without activating caspase-3. (C) 2010 Elsevier Masson SAS. All rights reserved.
dc.description.funderUniversidad Arturo Prat (UNAP)
dc.fechaingreso.objetodigital2024-04-16
dc.format.extent6 páginas
dc.fuente.origenWOS
dc.identifier.doi10.1016/j.ejmech.2010.10.006
dc.identifier.eissn1768-3254
dc.identifier.issn0223-5234
dc.identifier.pubmedidMEDLINE:20980080
dc.identifier.urihttps://doi.org/10.1016/j.ejmech.2010.10.006
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/75809
dc.identifier.wosidWOS:000285485000060
dc.information.autorucQuímica;Valderrama J ;S/I;98772
dc.issue.numero12
dc.language.isoen
dc.nota.accesocontenido parcial
dc.pagina.final6057
dc.pagina.inicio6052
dc.publisherELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
dc.revistaEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
dc.rightsacceso restringido
dc.subjectAntitumor agents
dc.subjectCytotoxicity
dc.subjectDonor-acceptor systems
dc.subjectQuinones
dc.subjectStructure-activity relationships
dc.subjectSUBSTITUTED 1,4-NAPHTHOQUINONES
dc.subjectOXIDATIVE STRESS
dc.subjectVITAMIN-C
dc.subjectDERIVATIVES
dc.subjectAPOPTOSIS
dc.subjectINHIBITION
dc.subjectHALLMARKS
dc.subjectPROTEINS
dc.subjectGROWTH
dc.subjectCANCER
dc.subject.ods03 Good Health and Well-being
dc.subject.odspa03 Salud y bienestar
dc.titleBiological evaluation of donor-acceptor aminonaphthoquinones as antitumor agents
dc.typeartículo
dc.volumen45
sipa.codpersvinculados98772
sipa.indexWOS
sipa.indexScopus
sipa.trazabilidadCarga SIPA;09-01-2024
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