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

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Ibrahim N,Mouawad L,Legraverend M

doi

10.1016/j.ejmech.2010.04.026

subject

Has Abstract

pub_date

2010-08-01 00:00:00

pages

3389-93

issue

8

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(10)00308-9

journal_volume

45

pub_type

杂志文章

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