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.

@article{Wagner2009DiscoveryO3,
  title={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.},
  author={Juergen Wagner and Peter von Matt and Richard Sedrani and Rainer Albert and Nigel G Cooke and Claus Ehrhardt and Martin Geiser and Gabriele Rummel and Wilhelm Stark and Andr{\'e} Strauss and Sandra W. Cowan-Jacob and Christian Beerli and Gisbert Weckbecker and Jean-Pierre Evenou and Gerhard Zenke and Sylvain Cottens},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 20},
  pages={6193-6}
}
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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