Indolyl-naphthyl-maleimides as potent and selective Inhibitors of Protein Kinase C-alpha/beta
Van Eis, Maurice, Evenou, Jean-Pierre, Schuler, Walter, Von Matt, Peter, Vangrevelinghe, Eric, 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 |