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 μM and 6 IC50 12.5 μM. Interestingly, the corresponding mono-ester derivatives of 3 showed no such selectivity.
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