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Hynes, Jr, John; Wu, Hong; Pitt, Sidney; Shen, Ding Ren; Zhang, Rosemary; Schieven, Gary L; Gillooly, Kathleen M; Shuster, David J; Taylor, Tracy L; Yang, XiaoXia; McIntyre, Kim W; McKinnon, Murray; Zhang, Hongjian; Marathe, Punit H; Doweyko, Arthur M; Kish, Kevin; Kiefer, Susan E; Sack, John S; Newitt, John A; Barrish, Joel C; Dodd, John; Leftheris, Katerina
Bioorganic & medicinal chemistry letters, 2008-Mar-15, 20080315, Volume: 18, Issue: 6Journal Article
A novel structural class of p38alpha MAP kinase inhibitors has been identified via iterative SAR studies of a focused deck screen hit. Optimization of the lead series generated 6e, BMS-640994, a potent and selective p38alpha inhibitor that is orally efficacious in rodent models of acute and chronic inflammation.
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