Identification of nonpeptidic small-molecule inhibitors of interleukin-2

…, W Lu, RS McDowell, HY Chul, BC Raimundo

Index: Waal, Nathan D.; Yang, Wenjin; Oslob, Johan D.; Arkin, Michelle R.; Hyde, Jennifer; Lu, Wanli; McDowell, Robert S.; Yu, Chul H.; Raimundo, Brian C. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 4 p. 983 - 987

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Citation Number: 27

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).