کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1379083 | 982017 | 2006 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Tricyclic azepine derivatives: Pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A novel class of pyrimido[4,5-b]-1,4-benzoxazepines is described as inhibitors of epidermal growth factor receptor (EGFR) tyrosine kinase. Two compounds display potent EGFR inhibitory activity of less than 1 μM in cellular phosphorylation assays (IC50 0.47–0.69 μM) and are highly selective against a small kinase panel. Such compounds demonstrate anti-EGFR activity within a class that is different from any known EGFR inhibitor scaffolds. They also provide a basis for the design of kinase inhibitors with the desired selectivity profile.
The synthesis and SAR studies of benzoxazepines as a novel EGFR kinase inhibitor class are reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 6, 15 March 2006, Pages 1643–1646
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 6, 15 March 2006, Pages 1643–1646
نویسندگان
Leon Smith II, Evgueni L. Piatnitski, Alexander S. Kiselyov, Xiaohu Ouyang, Xiaoling Chen, Sabina Burdzovic-Wizemann, Yongjiang Xu, Ying Wang, Robin L. Rosler, Sheetal N. Patel, Hui-Hsien Chiang, Daniel L. Milligan, John Columbus, Wai C. Wong,