Bioorganic and Medicinal Chemistry Letters p. 1643 - 1646 (2006)
Update date:2022-08-04
Topics:
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.
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.
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