کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376497 | 981959 | 2006 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors](/preview/png/1376497.png)
چکیده انگلیسی
The development of potent, orally bioavailable, and selective series of 5-amino-3-hydroxy-N(1-hydroxypropane-2-yl)isothiazole-4-carboxamidine inhibitors of MEK1 and MEK-2 kinase is described. Optimization of the carboxamidine and the phenoxyaniline group led to the identification of 55 which gave good potency as in vitro MEK1 inhibitors, and good oral exposure in rat.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 21, 1 November 2006, Pages 5561–5566
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 21, 1 November 2006, Pages 5561–5566
نویسندگان
Hassan El Abdellaoui, Chamakura V.N.S. Varaprasad, Dinesh Barawkar, Subrata Chakravarty, Andreas Maderna, Robert Tam, Huanming Chen, Matt Allan, Jim Z. Wu, Todd Appleby, Shunqi Yan, Weijian Zhang, Stanley Lang, Nanhua Yao, Robert Hamatake, Zhi Hong,