| Literature DB >> 16412636 |
Leon Smith1, Evgueni L Piatnitski, Alexander S Kiselyov, Xiaohu Ouyang, Xiaoling Chen, Sabina Burdzovic-Wizemann, Yongjiang Xu, Weitao Pan, Xin Chen, Ying Wang, Robin L Rosler, Sheetal N Patel, Hui-Hsien Chiang, Daniel L Milligan, John Columbus, Wai C Wong, Jacqueline F Doody, Yaron R Hadari.
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 microM in cellular phosphorylation assays (IC(50) 0.47-0.69 microM) 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.Entities:
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Year: 2006 PMID： 16412636 DOI： 10.1016/j.bmcl.2005.12.018
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823