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The first two cantharidin analogues displaying PP1 selectivity
Adam McCluskey1, Mirella A Keane, Cecilia C Walkom
1Medicinal Chemistry Group, School of Biological and Chemical Sciences, The University of Newcastle, University Drive, Callaghan, Newcastle, NSW 2308, Australia. amcclusk@mail.newcastle.edu.au
Bioorganic & Medicinal Chemistry Letters
|January 30, 2002
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 microM and 6 IC(50) 12.5 microM. Interestingly, the corresponding mono-ester derivatives of 3 showed no such selectivity.