کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365196 | 981554 | 2008 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Aryl–indolyl maleimides as inhibitors of CaMKIIδ. Part 1: SAR of the aryl region
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

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 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.
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 2390–2394
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 7, 1 April 2008, Pages 2390–2394
نویسندگان
Daniel E. Levy, Dan-Xiong Wang, Qing Lu, Zheng Chen, John Perumattam, Yong-jin Xu, Albert Liclican, Jeffrey Higaki, Hanmin Dong, Maureen Laney, Babu Mavunkel, Sundeep Dugar,