کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1361724 981470 2011 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of indazoles as inhibitors of Tpl2 kinase
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of indazoles as inhibitors of Tpl2 kinase
چکیده انگلیسی

Synthesis, modeling and structure–activity relationship of indazoles as inhibitors of Tpl2 kinase are described. From a high throughput screening effort, we identified an indazole hit compound 5 that has a single digit micromolar Tpl2 activity. Through SAR modifications at the C3 and C5 positions of the indazole, we discovered compound 31 with good potency in LANCE assay and cell-based p-Erk assay.

Synthesis, modeling and structure–activity relationship of indazoles as inhibitors of Tpl2 kinase are described. Through SAR modifications at the C3 and C5 positions of the indazole, we discovered compound 31 with good potency in LANCE assay (0.047 μM) and cell-based p-Erk assay (0.079 μM).Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 16, 15 August 2011, Pages 4758–4761
نویسندگان
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