Oxindole derivatives as inhibitors of TAK1 kinase

…, R Robinson, PA Ormonde, DM Cimbora…

Index: Lockman, Jeffrey W.; Reeder, Matthew D.; Robinson, Rosann; Ormonde, Patricia A.; Cimbora, Daniel M.; Williams, Brandi L.; Willardsen, J. Adam Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 6 p. 1724 - 1727

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Citation Number: 25

Abstract

Several series of oxindole analogues were synthesized and screened for inhibitory activity against transforming growth factor-β-activating kinase 1 (TAK1). Modifications around several regions of the lead molecules were made, with a distal hydroxyl group in the D region being critical for activity. The most potent compound 10 shows an IC50 of 8.9 nM against TAK1 in a biochemical enzyme assay, with compounds 3 and 6 showing low ...