Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3β
Copyright policy )Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3β
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-3beta 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.
- Korea Advanced Institute of Science and Technology Korea (Republic of)
- Konkuk University Korea (Republic of)
- Korea Advanced Institute of Science and Technology Korea (Republic of)
MECHANISM, Models, Molecular, Molecular Structure, Imidazoles, BETA, Benzene, PROTEIN-KINASE, Crystallography, X-Ray, MICE, Glycogen Synthase Kinase 3, Structure-Activity Relationship, Drug Design, SKELETAL-MUSCLE, Computer Simulation, Protein Kinase Inhibitors
MECHANISM, Models, Molecular, Molecular Structure, Imidazoles, BETA, Benzene, PROTEIN-KINASE, Crystallography, X-Ray, MICE, Glycogen Synthase Kinase 3, Structure-Activity Relationship, Drug Design, SKELETAL-MUSCLE, Computer Simulation, Protein Kinase Inhibitors
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