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  • The First Two Cantharidin Analogues Displaying PP1 Selectivity

    Author
    McCluskey, Adam
    A. Keane, Mirella
    C. Walkom, Cecilia
    C. Bowyer, Michael
    T. R. Sim, Alistar
    Young, David
    A. Sakoff, Jennette
    Year published
    2002
    Metadata
    Show full item record
    Abstract
    High pressure Diels-Alder reactions of furan and dimethylmaleate, and thiophene and maleimide resulted in two cantharidin analogues, 3 and 6 possessing PP1 selectivity (>40- and >30-fold selectivity) over PP2A. Both compounds exhibited moderate PP1 activity, 3 IC50 50 占and 6 IC50 12.5 卮 Interestingly, the corresponding mono-ester derivatives of 3 showed no such selectivity.High pressure Diels-Alder reactions of furan and dimethylmaleate, and thiophene and maleimide resulted in two cantharidin analogues, 3 and 6 possessing PP1 selectivity (>40- and >30-fold selectivity) over PP2A. Both compounds exhibited moderate PP1 activity, 3 IC50 50 占and 6 IC50 12.5 卮 Interestingly, the corresponding mono-ester derivatives of 3 showed no such selectivity.
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    Journal Title
    Bioorganic and Medicinal Chemistry Letters
    Volume
    12
    Issue
    3
    Publisher URI
    http://www.elsevier.com/wps/find/journaldescription.cws_home/972/description#description
    DOI
    https://doi.org/10.1016/S0960-894X(01)00777-6
    Copyright Statement
    © 2002 Elsevier : Reproduced in accordance with the copyright policy of the publisher : This journal is available online - use hypertext links
    Publication URI
    http://hdl.handle.net/10072/6960
    Collection
    • Journal articles

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