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

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

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 journal › Article

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 language	English
Pages (from-to)	391-393
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	12
Issue number	3
DOIs	https://doi.org/10.1016/S0960-894X(01)00777-6
Publication status	Published - 11 Feb 2002
Externally published	Yes

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McCluskey, A., Keane, M. A., Walkom, C. C., Bowyer, M. C., Sim, A. T. R., Young, D. J., & Sakoff, J. A. (2002). The first two cantharidin analogues displaying PP1 selectivity. Bioorganic and Medicinal Chemistry Letters, 12(3), 391-393. https://doi.org/10.1016/S0960-894X(01)00777-6

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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 μM and 6 IC50 12.5 μM. Interestingly, the corresponding mono-ester derivatives of 3 showed no such selectivity.",

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AU - McCluskey, Adam

AU - Keane, Mirella A.

AU - Walkom, Cecilia C.

AU - Bowyer, Michael C.

AU - Sim, Alistair T.R.

AU - Young, David J.

AU - Sakoff, Jennette A.

PY - 2002/2/11

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AB - 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.

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