Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596891 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
The identification, design, and synthesis of a series of novel sulfamide- and urea-based small-molecule antagonists of the protein-protein interaction IL-2/IL-2Rα are described. Installation of a furan carboxylic acid fragment onto a low-micromolar sulfamide resulted in a 23-fold improvement in activity, providing a sub-micromolar, nonpeptidic IL-2 inhibitor (IC50 = 0.60 μM).
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Authors
Nathan D. Waal, Wenjin Yang, Johan D. Oslob, Michelle R. Arkin, Jennifer Hyde, Wanli Lu, Robert S. McDowell, Chul H. Yu, Brian C. Raimundo,