کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1366718 981600 2007 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors
چکیده انگلیسی

A novel class of selective Tie-2 inhibitors was derived from a multi-kinase inhibitor 1. By reversing the amide connectivity and incorporating aminotriazine or aminopyridine hinge-binding moieties, excellent Tie-2 potency and KDR selectivity could be achieved with 3-substituted terminal aryl rings. X-ray co-crystal structure analysis aided inhibitor design. This series was evaluated on the basis of potency, selectivity, and rat pharmacokinetic parameters.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 10, 15 May 2007, Pages 2886–2889
نویسندگان
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