2. Academic Validation
  3. Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes

Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes

  • J Med Chem. 2009 Oct 22;52(20):6193-6. doi: 10.1021/jm901108b.
Jürgen Wagner 1,  Peter von Matt,  Richard Sedrani,  Rainer Albert,  Nigel Cooke,  Claus Ehrhardt,  Martin Geiser,  Gabriele Rummel,  Wilhelm Stark,  Andre Strauss,  Sandra W Cowan-Jacob,  Christian Beerli,  Gisbert Weckbecker,  Jean-Pierre Evenou,  Gerhard Zenke,  Sylvain Cottens
Affiliations

Affiliation

  • 1 Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland. juergen.wagner@novartis.com
PMID: 19827831 DOI: 10.1021/jm901108b
Abstract

A series of novel maleimide-based inhibitors of protein kinase C (PKC) were designed, synthesized, and evaluated. AEB071 (1) was found to be a potent, selective inhibitor of classical and novel PKC isotypes. 1 is a highly efficient immunomodulator, acting via inhibition of early T cell activation. The binding mode of maleimides to PKCs, proposed by molecular modeling, was confirmed by X-ray analysis of 1 bound in the active site of PKCalpha.

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