Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379083 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Abstract
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.
Graphical abstractThe synthesis and SAR studies of benzoxazepines as a novel EGFR kinase inhibitor class are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,