297745-47-2Relevant academic research and scientific papers
Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors
Wityak, John,Hobbs, Frank W.,Gardner, Daniel S.,Santella III, Joseph B.,Petraitis, Joseph J.,Sun, Jung-Hui,Favata, Margaret F.,Daulerio, Andrea J.,Horiuchi, Kurumi Y.,Copeland, Robert A.,Scherle, Peggy A.,Jaffe, Bruce D.,Trzaskos, James M.,Magolda, Ronald L.,Trainor, George L.,Duncia, John V.
, p. 1483 - 1486 (2004)
Employing phenylmalonitrile dianion chemistry, a large number of analogues of MEK inhibitor lead SH053 (IC50=140 nM) were rapidly synthesized leading to single digit nM inhibitors, displaying submicromolar AP-1 transcription inhibition in COS-7 cells. Compound 41, exhibiting a MEK IC 50=12 nM showed ip activity in a TPA-induced ear edema model with an ED50=5 mg/kg.
Amino-thio-acrylonitriles as MEK inhibitors
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Page column 22-23, (2010/02/05)
This invention relates generally to amino-thio-acrylonitriles of formula Ia or Ib: as MEK inhibitors, pharmaceutical compositions containing the same, and methods of using the same as for treatment and prevention of inflammatory disorders or as an antican
