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Indolyl-naphthyl-maleimides as potent and selective Inhibitors of Protein Kinase C-alpha/beta

Van Eis, Maurice and Evenou, Jean-Pierre and Schuler, Walter and Von Matt, Peter and Vangrevelinghe, Eric and Wagner, Juergen and Zenke, Gerhard (2017) Indolyl-naphthyl-maleimides as potent and selective Inhibitors of Protein Kinase C-alpha/beta. Bioorganic and medicinal chemistry letters, 27 (4). pp. 781-786. ISSN 1464-3405

Abstract

The indolyl-naphthyl maleimide 7 is a potent inhibitor of the classical PKC isotypes PKC-alpha/beta and shows excellent selectivity over the novel PKC isotypes delta, epsilon, eta and theta 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.

Item Type: Article
Date Deposited: 15 Mar 2017 00:45
Last Modified: 15 Mar 2017 00:45
URI: https://oak.novartis.com/id/eprint/31343

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