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https://locus.ufv.br//handle/123456789/12916
Tipo: | Artigo |
Título: | Synthesis of novel α-santonin derivatives as potential cytotoxic agents |
Autor(es): | Arantes, Francisco F.P. Barbosa, Luiz C.A. Maltha, Célia R.A. Demuner, Antônio J. Costa, PatriciaMarçal da Ferreira, José R.O. Costa-Lotufo, Letícia V. Moraes, Manoel O. Pessoa, Cláudia |
Abstract: | Ten novel a -santonin derivatives have been synthesized as cytotoxic agents. The in vitro antitumor activity of these compounds has been evaluated against cancer cells lines. Structure-activity relationships indicate that a -methylene- g -lactone and endoperoxide functionalities play important roles in conferring cytotoxicity. The compounds 2e4, possessing the a -methylene- g -lactone group showed IC 50 values between 5.70 and 16.40 m M. Mixture of isomers 5 and 6, with the a -methylene- g -lactone and endoperoxide functionalities, displayed the greatest activity, with IC 50 values between 1.45 and 4.35 m M. The biological assays conducted with normal cells revealed that the compounds 2, 5 and 6 are selective against cancer cells lines tested. Bioactive lactones described herein and in our previous report did not cause disruption of the cell membrane in mouse erythrocytes. |
Palavras-chave: | Parishin A synthesis Sesquiterpene lactones α-methylene-γ-lactone Endoperoxide bridge Cytotoxicity |
Editor: | European Journal of Medicinal Chemistry |
Tipo de Acesso: | Open Access |
URI: | https://doi.org/10.1016/j.ejmech.2010.10.003 http://www.locus.ufv.br/handle/123456789/12916 |
Data do documento: | 23-Out-2010 |
Aparece nas coleções: | Artigos |
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1-s2.0-S0223523410007439-main.pdf | texto completo | 215,58 kB | Adobe PDF | Visualizar/Abrir |
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