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https://locus.ufv.br//handle/123456789/19429
Tipo: | Artigo |
Título: | Novel hederagenin–triazolyl derivatives as potential anti-cancer agents |
Autor(es): | Rodríguez-Hernández, Diego Demuner, Antonio J. Barbosa, Luiz C.A. Heller, Lucie Csuk, René |
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. |
Palavras-chave: | Sapindus saponaria Huisgen 1,3-dipolar cycloaddition Hederagenin derivatives SRB assay |
Editor: | European Journal of Medicinal Chemistry |
Tipo de Acesso: | Elsevier Masson SAS. |
URI: | https://doi.org/10.1016/j.ejmech.2016.03.018 http://www.locus.ufv.br/handle/123456789/19429 |
Data do documento: | 10-Jun-2016 |
Aparece nas coleções: | Artigos |
Arquivos associados a este item:
Arquivo | Descrição | Tamanho | Formato | |
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artigo.pdf Until 2100-12-31 | texto completo | 819,33 kB | Adobe PDF | Visualizar/Abrir ACESSO RESTRITO |
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