Author/Authors :
Adam McCluskey، نويسنده , , Mirella A. Keane، نويسنده , , Cecilia C. Walkom، نويسنده , , Michael C. Bowyer، نويسنده , , Alistair T. R. Sim، نويسنده , , David J. Young، نويسنده , , Jennette A. Sakoff، نويسنده ,
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.
