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Eur J Med Chem. 2010 Aug;45(8):3389-93. doi: 10.1016/j.ejmech.2010.04.026. Epub 2010 Apr 28.

Novel 8-arylated purines as inhibitors of glycogen synthase kinase.

Author information

1
UMR 176 CNRS/Institut Curie, Bât. 110, Institut Curie, Centre Universitaire, 91405 Orsay, France.

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.

PMID:
20472330
DOI:
10.1016/j.ejmech.2010.04.026
[Indexed for MEDLINE]

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