Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate).

  title={Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate).},
  author={Hiroyuki Abe and Shinichi Kikuchi and Kazuhide Hayakawa and Tetsuya Iida and Noboru Nagahashi and Katsuya Maeda and Johei Sakamoto and Noriaki Matsumoto and Tomoya Miura and Koji Matsumura and Noriyoshi Seki and Takashi Inaba and Hisashi Kawasaki and Takayuki Yamaguchi and Reina Kakefuda and Toyomichi Nanayama and Hironori Kurachi and Yoshikazu Hori and Takayuki Yoshida and Junya Kakegawa and Yoshihiro Watanabe and Aidan G. Gilmartin and Mark C Richter and Katherine G. Moss and Sylvie G. Laquerre},
  journal={ACS medicinal chemistry letters},
  volume={2 4},
Inhibition of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) represents a promising strategy for the discovery of a new generation of anticancer chemotherapeutics. Our synthetic efforts, beginning from the lead compound 2, were directed at improving antiproliferative activity against cancer cells as well as various drug properties. These efforts led to the discovery of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7… CONTINUE READING
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5 - Amino - 2 , 4 , 7 - trioxo - 3 , 4 , 7 , 8 - tetrahydro - 2 H - pyrido - [ 2 , 3 - d ] - pyrimidine derivatives and related compounds for the treatment of cancer

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Bicyclic inhibitors of MEK and methods of use thereof

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