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Bioorg Med Chem Lett
; 21(6): 1724-7, 2011 Mar 15.
Article
in English
| MEDLINE
| ID: mdl-21316225
ABSTRACT
Several series of oxindole analogues were synthesized and screened for inhibitory activity against transforming growth factor-ß-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 IC(50) of 8.9 nM against TAK1 in a biochemical enzyme assay, with compounds 3 and 6 showing low micromolar cellular inhibition.