Literature DB >> 11814804

The first two cantharidin analogues displaying PP1 selectivity.

Adam McCluskey1, Mirella A Keane, Cecilia C Walkom, Michael C Bowyer, Alistair T R Sim, David J Young, Jennette A Sakoff.   

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.

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Year:  2002        PMID: 11814804     DOI: 10.1016/s0960-894x(01)00777-6

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


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