1505-58-4Relevant articles and documents
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 (2008/09/21)
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.
A new one step synthesis of maleimides by condensation of glyoxylate esters with acetamides
Faul, Margaret M.,Winneroski, Leonard L.,Krumrich, Christine A.
, p. 1109 - 1112 (2007/10/03)
Bisphenyl, bisheteroaryl, indolylaryl and indolylcycloalkyl maleimides are prepared in one step and 67-99% yield by condensation of glyoxylate esters with acetamides using a 1.0 M solution of potassium tert-butoxide in THF. The mechanism of the reaction is discussed.
