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. 2011 Jul 1;21(13):4066-71.
doi: 10.1016/j.bmcl.2011.04.121. Epub 2011 May 11.

Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase

Shaun R Selness  1 , Rajesh V Devraj, Balekudru Devadas, John K Walker, Terri L Boehm, Richard C Durley, Huey Shieh, Li Xing, Paul V Rucker, Kevin D Jerome, Alan G Benson, Laura D Marrufo, Heather M Madsen, Jeff Hitchcock, Tom J Owen, Lance Christie, Michele A Promo, Brian S Hickory, Edgardo Alvira, Win Naing, Radhika Blevis-Bal, Dean Messing, Jerry Yang, Michael K Mao, Gopi Yalamanchili, Richard Vonder Embse, Jeffrey Hirsch, Matthew Saabye, Sheri Bonar, Elizabeth Webb, Gary Anderson, Joseph B Monahan
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Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase

Shaun R Selness (V体育官网) et al. Bioorg Med Chem Lett. .

V体育2025版 - Abstract

The synthesis and SAR studies of a novel N-aryl pyridinone class of p38 kinase inhibitors are described VSports手机版. Systematic structural modifications to the HTS lead, 5, led to the identification of (-)-4a as a clinical candidate for the treatment of inflammatory diseases. Additionally, the chiral synthesis and properties of (-)-4a are described. .

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