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 | |
| Publication status | Published - 11 Feb 2002 |
| Externally published | Yes |
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The first two cantharidin analogues displaying PP1 selectivity. / McCluskey, Adam; Keane, Mirella A.; Walkom, Cecilia C.; Bowyer, Michael C.; Sim, Alistair T.R.; Young, David J.; Sakoff, Jennette A.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 12, No. 3, 11.02.2002, p. 391-393.Research output: Contribution to journal › Article › Research › peer-review
TY - JOUR
T1 - The first two cantharidin analogues displaying PP1 selectivity
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
Y1 - 2002/2/11
N2 - 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.
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.
UR - http://www.scopus.com/inward/record.url?scp=0037059906&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(01)00777-6
DO - 10.1016/S0960-894X(01)00777-6
M3 - Article
VL - 12
SP - 391
EP - 393
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 3
ER -