The First Two Cantharidin Analogues Displaying PP1 Selectivity
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.
View less >
View less >
Journal Title
Bioorganic and Medicinal Chemistry Letters
Volume
12
Issue
3
Publisher URI
Copyright Statement
© 2002 Elsevier : Reproduced in accordance with the copyright policy of the publisher : This journal is available online - use hypertext links