The first two cantharidin analogues displaying PP1 selectivity

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

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)391-393
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume12
Issue number3
DOIs
Publication statusPublished - 11 Feb 2002
Externally publishedYes

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