کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371429 981845 2011 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Oxindole derivatives as inhibitors of TAK1 kinase
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Oxindole derivatives as inhibitors of TAK1 kinase
چکیده انگلیسی

Several series of oxindole analogues were synthesized and screened for inhibitory activity against transforming growth factor-β-activating kinase 1 (TAK1). Modifications around several regions of the lead molecules were made, with a distal hydroxyl group in the D region being critical for activity. The most potent compound 10 shows an IC50 of 8.9 nM against TAK1 in a biochemical enzyme assay, with compounds 3 and 6 showing low micromolar cellular inhibition.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 6, 15 March 2011, Pages 1724–1727
نویسندگان
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