848411-85-8Relevant articles and documents
Identification of nonpeptidic small-molecule inhibitors of interleukin-2
Waal, Nathan D.,Yang, Wenjin,Oslob, Johan D.,Arkin, Michelle R.,Hyde, Jennifer,Lu, Wanli,McDowell, Robert S.,Yu, Chul H.,Raimundo, Brian C.
, p. 983 - 987 (2007/10/03)
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 (IC 50 = 0.60 μM).