کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371161 981839 2011 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors
چکیده انگلیسی

The insulin-like growth factor-1 receptor (IGF-1R) plays an important role in the regulation of cell growth and differentiation, and in protection from apoptosis. IGF-1R has been shown to be an appealing target for the treatment of human cancer. Herein, we report the synthesis, structure–activity relationships (SAR), X-ray cocrystal structure and in vivo tumor study results for a series of 2,4-bis-arylamino-1,3-pyrimidines.

The discovery of 2,4-bis-arylamino-1,3-pyrimidines as IGF-1R inhibitors is described. Optimization studies led to the identification of 26, which displayed tumor growth inhibition in a mouse Calu-6 tumor xenograft study.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 8, 15 April 2011, Pages 2394–2399
نویسندگان
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