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

• Published in: Bioorganic & medicinal chemistry letters Vol. 11; no. 5; pp. 635 - 639
• Main Authors: Smith, David G., Buffet, Marianne, Fenwick, Ashley E., Haigh, David, Ife, Robert J., Saunders, Martin, Slingsby, Brian P., Stacey, Rachel, Ward, Robert W.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 12.03.2001; Elsevier
• Subjects: Animals; Biological and medical sciences; 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; Medical sciences; Miscellaneous; Molecular Structure; Pharmacology. Drug treatments; Structure-Activity Relationship; Automation; Five membered ring; Enzyme; Nitrogen heterocycle; Transferases; Enzyme inhibitor; Selectivity; In vitro; Pyrrole derivatives; Imide; Structure activity relation; Protein kinase; Benzenic compound; Chemical synthesis; Secondary amine
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(00)00721-6

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. 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.