4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 9, Pages 2840-2844

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.03.079

Keywords

thiazolidine; Lyp; pTyr mimics; salicylate

Funding

  1. NHGRI NIH HHS [U54 HG003914-02, U54 HG003914, U54 HG003914-01, U54 HG003914-03] Funding Source: Medline

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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. (c) 2008 Elsevier Ltd. All rights reserved.

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