Inhibition of Caco-2 and MCF-7 cancer cells using chalcones: synthesis, biological evaluation and computational study

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dc.contributor.authorMellado, Marco
dc.contributor.authorReyna-Jeldes, Mauricio
dc.contributor.authorWeinstein-Oppenheimer, Caroline
dc.contributor.authorCoddou, Claudio
dc.contributor.authorJara-Gutierrez, Carlos
dc.contributor.authorVillena, Joan
dc.contributor.authorAguilar, Luis F.
dc.date.accessioned2022-11-30T02:47:10Z
dc.date.available2022-11-30T02:47:10Z
dc.date.issued2021
dc.description.abstractCancer is the second death cause worldwide, with breast and colon cancer among the most prevalent types. Traditional treatment strategies have several side effects that inspire the development of novel anticancer agents derived from natural sources, like chalcone derivatives. For this investigation, twenty-three chalcones (4a-w) were synthesized and evaluated as antiproliferative agents against MCF-7 and Caco-2 cells, finding three and two compounds with similar or higher antiproliferative activity than daunorubicin, while only two chalcones showed better selectivity indexes than daunorubicin on MCF-7. From these results, we developed good-performance QSAR models (r> 0.850, q2 >0.650), finding several structural features that could modify chalcone activity and selectivity. According to these models, chalcones 4w and 4t have high potency and selectivity against Caco-2 and MCF-7, respectively, which make them attractive candidates for hit-to-lead development of ROS-independent pro apoptotic agents.en_ES
dc.facultadFacultad de Medicinaen_ES
dc.file.nameWeinstein_Inhi2021.pdf
dc.identifier.citationMarco Mellado, Mauricio Reyna-Jeldes, Caroline Weinstein-Oppenheimer, Claudio Coddou, Carlos Jara-Gutierrez, Joan Villena & Luis F. Aguilar (2021): Inhibition of Caco-2 and MCF-7 cancer cells using chalcones: synthesis, biological evaluation and computational study, Natural Product Research, DOI: 10.1080/14786419.2021.1984465en_ES
dc.identifier.doihttps://doi.org/10.1080/14786419.2021.1984465
dc.identifier.urihttp://repositoriobibliotecas.uv.cl/handle/uvscl/7591
dc.languageen
dc.publisherTaylor & Francis
dc.sourceNatural Product Research
dc.subjectCHALCONEen_ES
dc.subjectBREAST CANCERen_ES
dc.subjectCOLON CANCERen_ES
dc.subjectSELECTIVITY INDEXen_ES
dc.subjectQUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPen_ES
dc.titleInhibition of Caco-2 and MCF-7 cancer cells using chalcones: synthesis, biological evaluation and computational study
dc.typeArticulo
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