Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3 beta

A hydroxy functional group was introduced as the hydrogen bond donor and acceptor at the hinge region of protein kinase in order to develop novel ATP-competitive inhibitors. Several derivatives of 7-hydroxyl-1H-benzoimidazole were designed as inhibitors of glycogen synthase kinase-3 beta with the help of ab initio calculations and a docking study. Enzymatic assay and an X-ray complex study showed that these designed compounds were highly potent ATP-competitive inhibitors. (c) 2007 Elsevier Ltd. All rights reserved.
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Issue Date
2007-10
Language
ENG
Keywords

SKELETAL-MUSCLE; PROTEIN-KINASE; MECHANISM; BETA; MICE

Citation

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.17, no.20, pp.5686 - 5689

ISSN
0960-894X
DOI
10.1016/j.bmcl.2007.07.056
URI
http://hdl.handle.net/10203/8225
Appears in Collection
NE-Journal Papers(저널논문)
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