Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors

…, G Bemis, F Salituro, M Ledeboer, E Harrington…

文献索引：Cao, Jingrong; Gao, Huai; Bemis, Guy; Salituro, Francesco; Ledeboer, Mark; Harrington, Edmund; Wilke, Susanne; Taslimi, Paul; Pazhanisamy; Xie, Xiaoling; Jacobs, Marc; Green, Jeremy Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 10 p. 2891 - 2895

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被引用次数: 23

摘要

A series of N-benzylated isatin oximes were developed as inhibitors of the mitogen-activated kinase, JNK3. X-ray crystallographic structures aided in the design and synthesis of novel, selective compounds, that inhibit JNK3, but not p38 MAP kinase and provided key insights into understanding the behavior of gatekeeper residue methionine-146 in determining target selectivity for this series.