1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.
Kenpaullone derivatives with a modified parent ring system were synthesized in order to develop kinase inhibitors with enhanced selectivity. Among the novel structures, 1-azakenpaullone was found to act as a selective GSK-3beta versus CDK1 inhibitor. The charge distribution within the 1-azakenpaullone molecule is discussed as a possible explanation for the enhanced GSK-3beta selectivity of 1-azakenpaullone compared to other paullone derivatives.
Kunick
Conrad
C
Institut für Pharmazeutische Chemie, Technische Universität Braunschweig, Beethovenstrasse 55, 38106, Braunschweig, Germany. kunick@chemie.uni-hamburg.de
Lauenroth
Kathrin
K
Leost
Maryse
M
Meijer
Laurent
L
Lemcke
Thomas
T
D001552:Benzazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000071679:Glycogen Synthase Kinase 3 beta; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology
D001552:Benzazepines; D004791:Enzyme Inhibitors; D007211:Indoles; C119620:kenpaullone; D000071679:Glycogen Synthase Kinase 3 beta; D038362:Glycogen Synthase Kinase 3