Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-α/β

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• 作者：Maurice J. van Eis ; ^{maurice.van_eis@novartis.com} ; JeanPierre Evenou ; Walter Schuler ; Gerhard Zenke ; Eric Vangrevelinghe ; Juergen Wagner ; Peter von Matt
• 关键词：PKC alpha/beta ; Inhibitors ; T-cell activation ; B-cell activation
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：27
• 期：4
• 页码：781-786
• 全文大小：1374 K
• 卷排序：27

文摘

The indolyl-naphthyl maleimide 7 is a potent inhibitor of the classical PKC isotypes α,β and shows excellent selectivity over the novel PKC isotypes δ,ε,η,θ and other kinases belonging to the AGC family. The SAR around 7 as well as the physico-chemical characteristics of selected derivatives and their activity in T and B cell activation and proliferation assays are discussed.