Novel 8-arylated purines as inhibitors of glycogen synthase kinase.
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Ibrahim N, Mouawad L, Legraverend M
Novel 8-arylated purines as inhibitors of glycogen synthase kinase.
Eur J Med Chem. 2010 Aug;45(8):3389-93. doi: 10.1016/j.ejmech.2010.04.026. Epub 2010 Apr 28.
- PubMed ID
- 20472330 [ View in PubMed]
- Abstract
A series of 8-arylated purine derivatives bearing either an aniline or an alkyl amide at position 6 were found to inhibit glycogen synthase kinase-3, with good selectivity over ten kinases. Molecular modeling studies indicated that the most active compounds (8a and 8e), adopt a planar conformation, close to the shape of AMPPNP in the crystal structure of GSK-3. These compounds are stabilized by hydrophobic contacts between the 8-aromatic group and the protein adenine pocket and by electrostatic contacts.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Staurosporine Glycogen synthase kinase-3 beta IC 50 (nM) 5 N/A N/A Details Staurosporine MAP kinase-activated protein kinase 2 IC 50 (nM) 36.25 N/A N/A Details