Novel hederagenin–triazolyl derivatives as potential anti-cancer agents

dc.creatorRodríguez-Hernández, Diego
dc.creatorDemuner, Antonio J.
dc.creatorBarbosa, Luiz C.A.
dc.creatorHeller, Lucie
dc.creatorCsuk, René
dc.date2018-05-09T18:24:39Z
dc.date2018-05-09T18:24:39Z
dc.date2016-06-10
dc.date.accessioned2023-09-27T21:50:33Z
dc.date.available2023-09-27T21:50:33Z
dc.identifier02235234
dc.identifierhttps://doi.org/10.1016/j.ejmech.2016.03.018
dc.identifierhttp://www.locus.ufv.br/handle/123456789/19429
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8966942
dc.descriptionA series of novel aryl-1H-1,2,3-triazol-4-yl methylester and amide derivatives of the natural product hederagenin was synthesized aiming to develop new antitumor agents, using Huisgen 1,3-dipolar cycloaddition reactions, with yields between 35% and 95%. The structures of all derivatives (2–31) were confirmed by MS, IR, ^1H NMR and ^13C NMR spectroscopic data. The cytotoxic activities of all compounds were screened against a panel of six human cancer cell lines using SRB assay. It was found that most of the compounds displayed higher levels of antitumor activities as compared to parent hederagenin. Compounds 4, 8 and 15 were the most potent against all human cancer cell lines. Furthermore, compound 11 was the most cytotoxic against cell HT29 showing EC50 = 1.6 μM and a selectivity index of 5.4.
dc.formatpdf
dc.formatapplication/pdf
dc.languageeng
dc.publisherEuropean Journal of Medicinal Chemistry
dc.relationv. 115, p. 257-267, june 2016
dc.rightsElsevier Masson SAS.
dc.subjectSapindus saponaria
dc.subjectHuisgen 1,3-dipolar cycloaddition
dc.subjectHederagenin derivatives
dc.subjectSRB assay
dc.titleNovel hederagenin–triazolyl derivatives as potential anti-cancer agents
dc.typeArtigo


Este ítem pertenece a la siguiente institución