Oxindole derivatives as inhibitors of TAK1 kinase |
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| Authors: | Lockman Jeffrey W Reeder Matthew D Robinson Rosann Ormonde Patricia A Cimbora Daniel M Williams Brandi L Willardsen J Adam |
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| Affiliation: | a Departments of Chemistry, Myrexis, Inc., 305 Chipeta Way, Salt Lake City, UT 84108, USA
b Discovery Biology, Myrexis, Inc., 305 Chipeta Way, Salt Lake City, UT 84108, USA |
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| 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 micromolar cellular inhibition. |
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| Keywords: | Kinase Oxindole TAK1 |
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