1024583-93-4Relevant academic research and scientific papers
Aryl-indolyl maleimides as inhibitors of CaMKIIδ. Part 1: SAR of the aryl region
Levy, Daniel E.,Wang, Dan-Xiong,Lu, Qing,Chen, Zheng,Perumattam, John,Xu, Yong-jin,Liclican, Albert,Higaki, Jeffrey,Dong, Hanmin,Laney, Maureen,Mavunkel, Babu,Dugar, Sundeep
, p. 2390 - 2394 (2008)
A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 34 nM to >20 μM and were dependant upon both the nature of the aryl group and the hydrogen bond donating potential of the maleimide ring. Key interactions with the kinase ATP site and hinge region were found to be consistent with homology modeling predictions.
Aryl-indolyl maleimides as inhibitors of CaMKIIδ. Part 2: SAR of the amine tether
Levy, Daniel E.,Wang, Dan-Xiong,Lu, Qing,Chen, Zheng,Perumattam, John,Xu, Yong-jin,Higaki, Jeffrey,Dong, Hanmin,Liclican, Albert,Laney, Maureen,Mavunkel, Babu,Dugar, Sundeep
, p. 2395 - 2398 (2008/09/20)
A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin-dependant kinase. Inhibitory activities against the enzyme ranged from 34 nM to >20 μM and were dependant upon both the nature of the aryl group and the tether joining the basic amine to the indolyl maleimide core. Key interactions with the kinase ATP site and hinge region, predicted by homology modeling, were confirmed.
