Novel hederagenin–triazolyl derivatives as potential anti-cancer agents

Show simple item record Rodríguez-Hernández, Diego Demuner, Antonio J. Barbosa, Luiz C.A. Heller, Lucie Csuk, René 2018-05-09T18:24:39Z 2018-05-09T18:24:39Z 2016-06-10
dc.identifier.issn 02235234
dc.description.abstract A 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. en
dc.format pdf pt-BR
dc.language.iso eng pt-BR
dc.publisher European Journal of Medicinal Chemistry pt-BR
dc.relation.ispartofseries v. 115, p. 257-267, june 2016 pt-BR
dc.rights Elsevier Masson SAS. pt-BR
dc.subject Sapindus saponaria pt-BR
dc.subject Huisgen 1,3-dipolar cycloaddition pt-BR
dc.subject Hederagenin derivatives pt-BR
dc.subject SRB assay pt-BR
dc.title Novel hederagenin–triazolyl derivatives as potential anti-cancer agents en
dc.type Artigo pt-BR

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