Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 1: SAR of the aryl region.
作者信息
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
机构信息
Scios, Inc., 6500 Paseo Padre Parkway, Fremont, CA 94555, USA.
出版信息
Bioorg Med Chem Lett. 2008 Apr 1;18(7):2390-4. doi: 10.1016/j.bmcl.2008.02.059. Epub 2008 Mar 4.
A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 34nM to >20microM 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.
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