The first two cantharidin analogues displaying PP1 selectivity

…, MA Keane, CC Walkom, MC Bowyer, ATR Sim…

Index: McCluskey, Adam; Keane, Mirella A.; Walkom, Cecilia C.; Bowyer, Michael C.; Sim, Alistair T.R.; Young, David J.; Sakoff, Jennette A. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 3 p. 391 - 393

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Citation Number: 57

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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