Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation.
作者信息
Lu Qing, Chen Zheng, Perumattam John, Wang Dan-Xiong, Liang Weiling, Xu Yong-Jin, Do Steven, Bonaga Llorente, Higaki Jeffrey, Dong Hanmin, Liclican Albert, Sideris Steve, Laney Maureen, Dugar Sundeep, Mavunkel Babu, Levy Daniel E
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):2399-403. doi: 10.1016/j.bmcl.2008.02.057. 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 10nM to >20microM and were dependant upon both the nature of the aryl group and the tether joining the basic amine to the indolyl maleimide core of the inhibitors. Key interactions with the kinase ATP site and hinge region, predicted by homology modeling, were confirmed.
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