652976-28-8Relevant academic research and scientific papers
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
LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS
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Page/Page column 311, (2008/06/13)
The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3β
Kunick, Conrad,Lauenroth, Kathrin,Leost, Maryse,Meijer, Laurent,Lemcke, Thomas
, p. 413 - 416 (2007/10/03)
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 (2007/10/03)
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
