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
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.
Journal Title
Bioorganic and Medicinal Chemistry Letters
Volume
12
Issue
3
Publisher URI
DOI
Copyright Statement
© 2002 Elsevier : Reproduced in accordance with the copyright policy of the publisher : This journal is available online - use hypertext links
Subject
Medicinal and Biomolecular Chemistry
Organic Chemistry
Pharmacology and Pharmaceutical Sciences
Publication URI
Collection