Studies on quinones. Part 46. Synthesis and in vitro antitumor evaluation of aminopyrimidoisoquinolinequinones

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dc.contributor.authorVasquez, David
dc.contributor.authorRodriguez, Jaime A.
dc.contributor.authorTheoduloz, Cristina
dc.contributor.authorCalderon, Pedro Buc
dc.contributor.authorValderrama, Jaime A.
dc.date.accessioned2024-01-10T12:08:54Z
dc.date.available2024-01-10T12:08:54Z
dc.date.issued2010
dc.description.abstractIn the search of structure-activity relationship studies and to explore the antitumor effect associated with the pyrimidoisoquinolinequinone scaffold, several diversily substituted 8-aminopyrimido[4,5-c] isoquinolinequinones were regioselectively synthesized. Variation in the structure of the nitrogen substituent bonded to the 8-position of the pyrimidoisoquinolinequinone system led to a set of alkylamino-, phenylamino- and alkyphenylamino derivatives. The cytotoxic activity of the aminoquinone derivatives was evaluated in vitro using the MTT colorimetric method against one normal cell line (MRCS lung fibroblasts) and four human cancer cell lines (AGS human gastric adenocarcinoma; SK-MES-1 human lung cancer cells, and J82 human bladder carcinoma; HL-60 human leukemia) in 72-h drug exposure assays. Among the series, five compounds exhibited interesting antitumor activity against AGS human gastric adenocarcinoma and human lung cancer cells. The SAR studies revealed that both the nature of the nitrogen substituent into the quinone ring and the methyl group at the 6-position play key roles in the antitumor activity. (C) 2010 Elsevier Masson SAS. All rights reserved.
dc.description.funderFondo Nacional de Ciencia y Tecnologia
dc.fechaingreso.objetodigital2024-04-16
dc.format.extent9 páginas
dc.fuente.origenWOS
dc.identifier.doi10.1016/j.ejmech.2010.08.040
dc.identifier.eissn1768-3254
dc.identifier.issn0223-5234
dc.identifier.pubmedidMEDLINE:20828890
dc.identifier.urihttps://doi.org/10.1016/j.ejmech.2010.08.040
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/76439
dc.identifier.wosidWOS:000283911300065
dc.information.autorucQuímica; Vasquez D;S/I;117510
dc.information.autorucQuímica;Valderrama JA ;S/I;98772
dc.issue.numero11
dc.language.isoen
dc.nota.accesocontenido parcial
dc.pagina.final5242
dc.pagina.inicio5234
dc.publisherELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
dc.revistaEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
dc.rightsacceso restringido
dc.subjectAminopyrimido[4,5-c]isoquinolinequinones
dc.subjectNucleophilic substitution
dc.subjectAntitumor activity
dc.subjectMTT assay
dc.subjectSAR analysis
dc.subjectCELL-LINES
dc.subjectREGIOSELECTIVITY
dc.subjectANALOGS
dc.subjectAGENTS
dc.subjectASSAY
dc.subject.ods03 Good Health and Well-being
dc.subject.odspa03 Salud y bienestar
dc.titleStudies on quinones. Part 46. Synthesis and in vitro antitumor evaluation of aminopyrimidoisoquinolinequinones
dc.typeartículo
dc.volumen45
sipa.codpersvinculados117510
sipa.codpersvinculados98772
sipa.indexWOS
sipa.indexScopus
sipa.trazabilidadCarga SIPA;09-01-2024
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