3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3)

D G Smith; M Buffet; A E Fenwick; D Haigh; R J Ife; M Saunders; B P Slingsby; R Stacey; R W Ward

doi:10.1016/s0960-894x(00)00721-6

3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3)

Bioorg Med Chem Lett. 2001 Mar 12;11(5):635-9. doi: 10.1016/s0960-894x(00)00721-6.

Authors

D G Smith¹, M Buffet, A E Fenwick, D Haigh, R J Ife, M Saunders, B P Slingsby, R Stacey, R W Ward

Affiliation

¹ SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK. dave_g_smith@sbphrd.com

PMID: 11266159
DOI: 10.1016/s0960-894x(00)00721-6

Abstract

Potent 3-anilino-4-arylmaleimide glycogen synthase kinase-3 (GSK-3) inhibitors have been prepared using automated array methodology. A number of these are highly selective, having little inhibitory potency against more than 20 other protein kinases.

MeSH terms

Animals
Bipolar Disorder / drug therapy
Calcium-Calmodulin-Dependent Protein Kinases / antagonists & inhibitors*
Calcium-Calmodulin-Dependent Protein Kinases / metabolism
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Enzyme Inhibitors / therapeutic use
Glycogen Synthase Kinases
Humans
Maleimides / chemical synthesis
Maleimides / chemistry
Maleimides / pharmacology*
Maleimides / therapeutic use
Molecular Structure
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Maleimides
Glycogen Synthase Kinases
Calcium-Calmodulin-Dependent Protein Kinases