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

  • Bioorg Med Chem Lett. 2017 Feb 15;27(4):781-786. doi: 10.1016/j.bmcl.2017.01.038.
Maurice J van Eis  1 ,  JeanPierre Evenou  2 ,  Walter Schuler  2 ,  Gerhard Zenke  2 ,  Eric Vangrevelinghe  2 ,  Juergen Wagner  2 ,  Peter von Matt  2
Affiliations
  • 1. Novartis Institutes for BioMedical Research, Forum 1, Novartis Campus, CH-4056 Basel, Switzerland. Electronic address: [email protected].
  • 2. Novartis Institutes for BioMedical Research, Forum 1, Novartis Campus, CH-4056 Basel, Switzerland.
PMID: 28131714 DOI: 10.1016/j.bmcl.2017.01.038
Abstract

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.

Keywords
B-cell activation; Inhibitors; PKC alpha/beta; T-cell activation.