- Aryl-indolyl maleimides as inhibitors of CaMKIIδ. Part 1: SAR of the aryl region
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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.
- 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
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p. 2390 - 2394
(2008/09/21)
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- DRUGS INHIBITING CELL DEATH
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A cell death inhibitor, a pharmaceutical or a preservative for organs, tissues or cells, a comprising, as an active ingredient, an indolylmaleimide derivative represented by the following formula (I), which is useful for inhibiting death of cells, the drug being expected as a preventive or a remedy for the progress of various diseases wherein cell death participates in progress and exacerbation thereof:
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- A new one step synthesis of maleimides by condensation of glyoxylate esters with acetamides
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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.
- Faul, Margaret M.,Winneroski, Leonard L.,Krumrich, Christine A.
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p. 1109 - 1112
(2007/10/03)
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