The First Two Cantharidin Analogues Displaying PP1 Selectivity

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Author(s)
McCluskey, Adam
A. Keane, Mirella
C. Walkom, Cecilia
C. Bowyer, Michael
T. R. Sim, Alistar
Young, David
A. Sakoff, Jennette
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Dr DL Boger

Date
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.

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Bioorganic and Medicinal Chemistry Letters

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12

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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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Medicinal and Biomolecular Chemistry

Organic Chemistry

Pharmacology and Pharmaceutical Sciences

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