کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365723 | 981570 | 2007 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3β
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A hydroxy functional group was introduced as the hydrogen bond donor and acceptor at the hinge region of protein kinase in order to develop novel ATP-competitive inhibitors. Several derivatives of 7-hydroxyl-1H-benzoimidazole were designed as inhibitors of glycogen synthase kinase-3β with the help of ab initio calculations and a docking study. Enzymatic assay and an X-ray complex study showed that these designed compounds were highly potent ATP-competitive inhibitors.
We have designed new kinase inhibitors by considering the hydrogen bond network in the hinge region and confirmed through the enzymatic assay and X-ray crystallography.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 20, 15 October 2007, Pages 5686–5689
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 20, 15 October 2007, Pages 5686–5689
نویسندگان
Dongkyu Shin, Seung-Chul Lee, Yong-Seok Heo, Woon-Young Lee, Yong-Soon Cho, Yong Eun Kim, Young-Lan Hyun, Joong Myung Cho, Yoon Sup Lee, Seonggu Ro,