| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373482 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
A potent and selective series of 2-amino-3,5-diarylbenzamide inhibitors of IKK-α and IKK-β is described. The most potent compounds are 8h, 8r and 8v, with IKK-β inhibitory potencies of pIC50 7.0, 6.8 and 6.8, respectively. The series has excellent selectivity, both within the IKK family over IKK-ε, and across a wide variety of kinase assays. The potency of 8h in the IKK-β enzyme assay translates to significant cellular activity (pIC50 5.7–6.1) in assays of functional and mechanistic relevance.
Graphical abstractA potent and selective series of 2-amino-3,5-diarylbenzamide inhibitors of IKK-α and IKK-β is described. The most potent compounds are 8h, 8r and 8v, with IKK-β inhibitory potencies of pIC50 7.0, 6.8 and 6.8, respectively. The series has excellent selectivity, both within the IKK family over IKK-ε, and across a wide variety of kinase assays. The potency of 8h in the IKK-α and IKK-β enzyme assay translates to significant cellular activity (pIC50 5.7–6.1) in assays of functional and mechanistic relevance.Figure optionsDownload full-size imageDownload as PowerPoint slide
