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  • Title: Synthesis of novel α-santonin derivatives as potential cytotoxic agents.
    Author: Arantes FF, Barbosa LC, Maltha CR, Demuner AJ, Marçal da Costa P, Ferreira JR, Costa-Lotufo LV, Moraes MO, Pessoa C.
    Journal: Eur J Med Chem; 2010 Dec; 45(12):6045-51. PubMed ID: 20971532.
    Abstract:
    Ten novel α-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 α-methylene-γ-lactone and endoperoxide functionalities play important roles in conferring cytotoxicity. The compounds 2-4, possessing the α-methylene-γ-lactone group showed IC50 values between 5.70 and 16.40 μM. Mixture of isomers 5 and 6, with the α-methylene-γ-lactone and endoperoxide functionalities, displayed the greatest activity, with IC50 values between 1.45 and 4.35 μM. 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.
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