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
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 16, 15 August 2011, Pages 4758–4761
نویسندگان
Yonghan Hu, Derek Cole, Rajiah Aldrin Denny, David R. Anderson, Manus Ipek, Yike Ni, Xiaolun Wang, Suvit Thaisrivongs, Timothy Chamberlain, J. Perry Hall, Julie Liu, Michael Luong, Lih-Ling Lin, Jean-Baptiste Telliez, Ariamala Gopalsamy,