Use este identificador para citar ou linkar para este item: 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
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