کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10591919 981769 2013 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors
چکیده انگلیسی
Drug design efforts in the emerging 2-aminothiazole-4-carboxamide class of CHK1 inhibitors have uncovered specific combinations of key substructures within the molecule; resulting in significant improvements in cell-based activity while retaining a greater than one hundred-fold selectivity against CDK2. The X-ray crystal structure of a complex between compound 39 and the CHK1 protein detailing a 'U-shaped' topology and key interactions with the protein surface at the ATP site is also reported.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 9, 1 May 2013, Pages 2590-2594
نویسندگان
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