کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376239 | 981952 | 2008 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: Design, synthesis, and biological activity
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A novel series of 7-[1H-indol-2-yl]-2,3-dihydro-isoindol-1-ones designed to be inhibitors of VEGF-R2 kinase was synthesized and found to potently inhibit VEGF-R2 and Aurora-A kinases. The structure-based design, synthesis, and initial SAR of the series are discussed.
The design of a new kinase inhibitor scaffold 1 based on known VEGF-R2 kinase inhibitors is described. The series designed to be inhibitors of VEGF-R2 kinase were synthesized and found to potently inhibit VEGF-R2 and Aurora-A kinases. The structure-based design, synthesis, initial SAR, and in vivo efficacy of the series are discussed.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 18, 15 September 2008, Pages 5130–5133
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 18, 15 September 2008, Pages 5130–5133
نویسندگان
Terry V. Hughes, Stuart L. Emanuel, Harold R. O’Grady, Peter J. Connolly, Catherine Rugg, Angel R. Fuentes-Pesquera, Prabha Karnachi, Richard Alexander, Steven A. Middleton,