- Title
- The first two cantharidin analogues displaying PP1 selectivity
- Creator
- McCluskey, Adam; Keane, Mirella A.; Walkom, Cecilia C.; Bowyer, Michael C.; Sim, Alistair T. R.; Young, David J.; Sakoff, Jennette A.
- 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
- Publisher
- Elsevier Science Ltd.
- Resource Type
- journal article
- Date
- 2002
- 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.
- Subject
- Diels-Alder reactions; furan; dimethylmaleate; PP1 selectivity; thiophene; maleimide
- Identifier
- http://hdl.handle.net/1959.13/33856
- Identifier
- uon:3324
- Identifier
- ISSN:0960-894X
- Language
- eng
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