ChemInform Abstract: The First Two Cantharidin Analogues Displaying PP1 Selectivity

Authors :: Alistair T. R. Sim
Jennette A. Sakoff
Michael C. Bowyer
Adam McCluskey
David J. Young
Cecilia C. Walkom
Mirella A. Keane
Source :: ChemInform. 33
Publication Year :: 2010
Publisher :: Wiley, 2010.
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 IC 50 50 μM and 6 IC 50 12.5 μM. Interestingly, the corresponding mono-ester derivatives of 3 showed no such selectivity.

Subjects :: chemistry.chemical_compound
Cantharidin
chemistry
Furan
High pressure
Thiophene
General Medicine
Selectivity
Thiophene derivatives
Maleimide
Medicinal chemistry

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