| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371429 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
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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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jeffrey W. Lockman, Matthew D. Reeder, Rosann Robinson, Patricia A. Ormonde, Daniel M. Cimbora, Brandi L. Williams, J. Adam Willardsen,