Discovery of a novel submicromolar inhibitor of the lymphoid specific tyrosine phosphatase

作者:Xie Yuli; Liu Yidong; Gong Gangli; Rinderspacher Alison; Deng Shi Xian; Smith Deborah H; Toebben Udo; Tzilianos Effie; Branden Lars; Vidovic Dusica; Chung Caty; Schurer Stephan; Tautz Lutz; Landry Donald W*
来源:Bioorganic & Medicinal Chemistry Letters, 2008, 18(9): 2840-2844.
DOI:10.1016/j.bmcl.2008.03.079

摘要

We report here a class of thiazolidine-2,4-diones and 2-thioxothiazolidin-4-ones as potent inhibitors of the lymphoid specific tyrosine phosphatase (Lyp) identified from high throughput screens. Chemical modi. cation by incorporating the known phosphotyrosine (pTyr) mimics led to the discovery of a salicylate-based inhibitor with submicromolar potency.