The First Two Cantharidin Analogues Displaying PP1 Selectivity

McCluskey, Adam; A. Keane, Mirella; C. Walkom, Cecilia; C. Bowyer, Michael; T. R. Sim, Alistar; Young, David; A. Sakoff, Jennette

doi:10.1016/S0960-894X(01)00777-6

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Year published

2002

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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 占and 6 IC50 12.5 卮 Interestingly, the corresponding mono-ester derivatives of 3 showed no such selectivity.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 占and 6 IC50 12.5 卮 Interestingly, the corresponding mono-ester derivatives of 3 showed no such selectivity.
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Bioorganic and Medicinal Chemistry Letters

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http://www.elsevier.com/wps/find/journaldescription.cws_home/972/description#description

DOI

https://doi.org/10.1016/S0960-894X(01)00777-6

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http://hdl.handle.net/10072/6960

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Journal articles