425636-74-4Relevant academic research and scientific papers
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
Wagner, Jürgen,Von Matt, Peter,Sedrani, Richard,Albert, Rainer,Cooke, Nigel,Ehrhardt, Claus,Geiser, Martin,Rummel, Gabriele,Stark, Wilhelm,Strauss, Andre,Cowan-Jacob, Sandra W.,Beerli, Christian,Weckbecker, Gisbert,Evenou, Jean-Pierre,Zenke, Gerhard,Cottens, Sylvain
supporting information; experimental part, p. 6193 - 6196 (2010/04/02)
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 PKCα. 2009 American Chemical Society.
