Structure-based design and parallel synthesis of N
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- 作者：Jingrong Cao ; Huai Gao ; Guy Bemis ; Francesco Salituro ; Mark Ledeboer ; Edmund Harrington ; Susanne Wilke ; Paul Taslimi ; S. Pazhanisamy ; Xiaoling Xie ; Marc Jacobs ; Jeremy Green
- 关键词：JNK3 ; JNK3 inhibitors ; MAP kinase ; Isatin
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：15 May 2009
- 年：2009
- 卷：19
- 期：10
- 页码：2891-2895
- 全文大小：857 K
文摘
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.