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

…, U Toebben, E Tzilianos, L Branden, D Vidović…

Index: Xie, Yuli; Liu, Yidong; Gong, Gangli; Rinderspacher, Alison; Deng, Shi-Xian; Smith, Deborah H.; Toebben, Udo; Tzilianos, Effie; Branden, Lars; Vidovic, Dusica; Chung, Caty; Schuerer, Stephan; Tautz, Lutz; Landry, Donald W. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 9 p. 2840 - 2844

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Citation Number: 33

Abstract

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 modification by incorporating the known phosphotyrosine (pTyr) mimics led to the discovery of a salicylate-based inhibitor with submicromolar potency.