875926-22-0Relevant articles and documents
Tricyclic azepine derivatives: Pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors
Smith II, Leon,Piatnitski, Evgueni L.,Kiselyov, Alexander S.,Ouyang, Xiaohu,Chen, Xiaoling,Burdzovic-Wizemann, Sabina,Xu, Yongjiang,Wang, Ying,Rosler, Robin L.,Patel, Sheetal N.,Chiang, Hui-Hsien,Milligan, Daniel L.,Columbus, John,Wong, Wai C.,Doody, Jacqueline F.,Hadari, Yaron R.
, p. 1643 - 1646 (2007/10/03)
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.
