The first two cantharidin analogues displaying PP1 selectivity | NOVA. The University of Newcastle's Digital Repository

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Please use this identifier to cite or link to this item: http://hdl.handle.net/1959.13/33856

Title: The first two cantharidin analogues displaying PP1 selectivity
Author/Creator: McCluskey, Adam; Keane, Mirella A.; Walkom, Cecilia C.; Bowyer, Michael C.; Sim, Alistair T. R.; Young, David J.; Sakoff, Jennette A.
Institution: The University of Newcastle. Faculty of Engineering & Built Environment, School of Engineering
Description: 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.
Relation: Bioorganic & Medicinal Chemistry Letters Vol. 12, Issue 3, p. 391-393
Publisher Link: http://dx.doi.org/10.1016/S0960-894X(01)00777-6
Date: 2002
Publisher: Elsevier Science Ltd.
Keyword(s): Diels-Alder reactions; furan; dimethylmaleate; PP1 selectivity; thiophene; maleimide
Resource Type: journal article
Identifier: http://hdl.handle.net/1959.13/33856
Identifier: ISSN:0960-894X

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