کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1365197 981554 2008 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Aryl-indolyl maleimides as inhibitors of CaMKIIδ. Part 2: SAR of the amine tether
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Aryl-indolyl maleimides as inhibitors of CaMKIIδ. Part 2: SAR of the amine tether
چکیده انگلیسی

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.

Aryl-substituted maleimides were prepared and studied for their activity against CaMKIIδ. Inhibitory activities ranged from 34 nM to >20 μM. Key predicted interactions with the kinase ATP site and hinge region were confirmed.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 7, 1 April 2008, Pages 2395–2398
نویسندگان
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