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

[Display omitted] 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 d...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-02, Vol.27 (4), p.781-786
Hauptverfasser:	van Eis, Maurice J., Evenou, JeanPierre, Schuler, Walter, Zenke, Gerhard, Vangrevelinghe, Eric, Wagner, Juergen, von Matt, Peter
Format:	Artikel
Sprache:	eng
Schlagworte:	B-cell activation B-Lymphocytes - cytology B-Lymphocytes - drug effects B-Lymphocytes - metabolism Binding Sites Cell Proliferation - drug effects Humans Indoles - chemistry Inhibitors Inhibitory Concentration 50 Isoenzymes - antagonists & inhibitors Isoenzymes - metabolism Lymphocyte Activation - drug effects Maleimides - chemical synthesis Maleimides - chemistry Maleimides - pharmacology Molecular Docking Simulation Naphthols - chemistry PKC alpha/beta Protein Binding Protein Kinase C beta - antagonists & inhibitors Protein Kinase C beta - metabolism Protein Kinase C-alpha - antagonists & inhibitors Protein Kinase C-alpha - metabolism Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein Structure, Tertiary Structure-Activity Relationship T-cell activation T-Lymphocytes - cytology T-Lymphocytes - drug effects T-Lymphocytes - metabolism
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Zusammenfassung:	[Display omitted] 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2017.01.038