UM
Tricyclic azepine derivatives: Pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors
Smith II L.1; Piatnitski E.L.1; Kiselyov A.S.1; Ouyang X.1; Chen X.1; Burdzovic-Wizemann S.1; Xu Y.1; Wang Y.1; Rosler R.L.1; Patel S.N.1; Chiang H.-H.1; Milligan D.L.1; Columbus J.1; Wong W.C.1; Doody J.F.1; Hadari Y.R.1
2006-03-15
Source PublicationBioorganic and Medicinal Chemistry Letters
ISSN0960894X
Volume16Issue:6Pages:1643-1646
AbstractA 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 (IC 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. © 2005 Elsevier Ltd. All rights reserved.
KeywordBenzoxazepine Epidermal growth factor receptor Kinase inhibitor Kinase selectivity
DOI10.1016/j.bmcl.2005.12.018
URLView the original
Language英語
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Cited Times [WOS]:18   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.Eli Lilly and Company
2.ChemDiv, Inc.
3.Bristol-Myers Squibb
Recommended Citation
GB/T 7714
Smith II L.,Piatnitski E.L.,Kiselyov A.S.,et al. Tricyclic azepine derivatives: Pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors[J]. Bioorganic and Medicinal Chemistry Letters,2006,16(6):1643-1646.
APA Smith II L..,Piatnitski E.L..,Kiselyov A.S..,Ouyang X..,Chen X..,...&Hadari Y.R..(2006).Tricyclic azepine derivatives: Pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors.Bioorganic and Medicinal Chemistry Letters,16(6),1643-1646.
MLA Smith II L.,et al."Tricyclic azepine derivatives: Pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors".Bioorganic and Medicinal Chemistry Letters 16.6(2006):1643-1646.
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