652976-27-7Relevant academic research and scientific papers
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3β
Kunick, Conrad,Lauenroth, Kathrin,Leost, Maryse,Meijer, Laurent,Lemcke, Thomas
, p. 413 - 416 (2004)
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-3β versus CDK1 inhibitor. The charge distribution within the 1-azakenpaullone molecule is discussed as a possible explanation for the enhanced GSK-3β selectivity of 1-azakenpaullone compared to other paullone derivatives.
Evaluation and Comparison of 3D-QSAR CoMSIA Models for CDK1, CDK5, and GSK-3 Inhibition by Paullones
Kunick, Conrad,Lauenroth, Kathrin,Wieking, Karen,Xie, Xu,Schultz, Christiane,Gussio, Rick,Zaharevitz, Daniel,Leost, Maryse,Meijer, Laurent,Weber, Alexander,J?rgensen, Flemming S.,Lemcke, Thomas
, p. 22 - 36 (2004)
With a view to the rational design of selective GSK-3β inhibitors, 3D-QSAR CoMSIA models were developed for the inhibition of the three serine/threonine kinases CDK1/cyclin B, CDK5/p25, and GSK-3β by compounds from the paullone inhibitor family. The model
9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma
Maiwald, Franziska,Benítez, Diego,Charquero, Diego,Dar, Mahin Abad,Erdmann, Hanna,Preu, Lutz,Koch, Oliver,H?lscher, Christoph,Loa?c, Nadège,Meijer, Laurent,Comini, Marcelo A.,Kunick, Conrad
, p. 274 - 283 (2014/07/08)
Trypanosomes from the "brucei" complex are pathogenic parasites endemic in sub-Saharan Africa and causative agents of severe diseases in humans and livestock. In order to identify new antitrypanosomal chemotypes against African trypanosomes, 4-azapaullone
