N-(3-Cyano-4, 5, 6, 7-tetrahydro-1-benzothien-2-yl) amides as potent, selective, inhibitors of JNK2 and JNK3

…, TT Chuang, JA Christopher, M Cichy-Knight…

Index: Angell, Richard M.; Atkinson, Francis L.; Brown, Murray J.; Chuang, Tsu Tshen; Christopher, John A.; Cichy-Knight, Maria; Dunn, Allison K.; Hightower, Kendra E.; Malkakorpi, Susanna; Musgrave, James R.; Neu, Margarete; Rowland, Paul; Shea, Robyn L.; Smith, Jeffery L.; Somers, Donald O.; Thomas, Sonia A.; Thompson, Gladstone; Wang, Ruolan Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1296 - 1301

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Citation Number: 53

Abstract

The identification and exploration of a novel, potent and selective series of N-(3-cyano-4, 5, 6, 7-tetrahydro-1-benzothien-2-yl) amide inhibitors of JNK2 and JNK3 kinases is described. Compounds 5a and 11a were identified as potent inhibitors of JNK3 (pIC50 6.7 and 6.6, respectively), with essentially equal potency against JNK2 (pIC50 6.5). Selectivity within the mitogen-activated protein kinase (MAPK) family, against JNK1, p38α and ERK2, was ...