The First Two Cantharidin Analogues Displaying PP1 Selectivity

Author(s)
McCluskey, Adam
A. Keane, Mirella
C. Walkom, Cecilia
C. Bowyer, Michael
T. R. Sim, Alistar
Young, David
A. Sakoff, Jennette
Griffith University Author(s)
Year published
2002
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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.
Journal Title
Bioorganic and Medicinal Chemistry Letters
Volume
12
Issue
3
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© 2002 Elsevier : Reproduced in accordance with the copyright policy of the publisher : This journal is available online - use hypertext links
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