eprintid: 20495 rev_number: 24 userid: 1419 dir: disk0/00/02/04/95 datestamp: 2014-02-13 23:18:15 lastmod: 2021-06-12 22:55:52 status_changed: 2014-02-13 23:18:15 type: article metadata_visibility: show item_issues_count: 0 eprint_status: archive creators_name: Wipf, P creators_name: Aslan, DC creators_name: Southwick, EC creators_name: Lazo, JS creators_email: pwipf@pitt.edu creators_email: creators_email: creators_email: creators_id: PWIPF creators_id: creators_id: creators_id: title: Sulfonylated aminothiazoles as new small molecule inhibitors of protein phosphatases ispublished: pub divisions: sch_as_chemistry full_text_status: public abstract: Based on a previously identified lead structure, SC-ααδ9, we have developed a versatile new chemical scaffold that can be readily modified to generate libraries of both Tyr and dual specificity phosphatase inhibitors with reduced molecular weight and lipophilicity. The most potent analogue identified to date, aminothiazole 8z, inhibits the dual specificity phosphatase Cdc25B with a Ki of 4.6 ± 0.4 μM and a Hill coefficient of 2. © 2001 Elsevier Science Ltd. date: 2001-02-12 date_type: published publication: Bioorganic and Medicinal Chemistry Letters volume: 11 number: 3 pagerange: 313 - 317 refereed: TRUE issn: 0960-894X id_number: 10.1016/S0960-894X(00)00658-2 pmid: 11212099 mesh_headings: Cell Cycle Proteins--antagonists & inhibitors mesh_headings: Combinatorial Chemistry Techniques mesh_headings: Dual Specificity Phosphatase 3 mesh_headings: Enzyme Inhibitors--chemical synthesis mesh_headings: Enzyme Inhibitors--pharmacology mesh_headings: Humans mesh_headings: Inhibitory Concentration 50 mesh_headings: Phosphoprotein Phosphatases--antagonists & inhibitors mesh_headings: Protein Tyrosine Phosphatase, Non-Receptor Type 1 mesh_headings: Protein Tyrosine Phosphatases--antagonists & inhibitors mesh_headings: Structure-Activity Relationship mesh_headings: Sulfonic Acids--chemical synthesis mesh_headings: Sulfonic Acids--pharmacology mesh_headings: Thiazoles--chemical synthesis mesh_headings: Thiazoles--pharmacology mesh_headings: cdc25 Phosphatases--antagonists & inhibitors chemical_names: Cell Cycle Proteins chemical_names: Enzyme Inhibitors chemical_names: Sulfonic Acids chemical_names: Thiazoles chemical_names: sulfamic acid chemical_names: CDC25B protein, human chemical_names: Phosphoprotein Phosphatases chemical_names: DUSP3 protein, human chemical_names: Dual Specificity Phosphatase 3 chemical_names: PTPN1 protein, human chemical_names: Protein Tyrosine Phosphatase, Non-Receptor Type 1 chemical_names: Protein Tyrosine Phosphatases chemical_names: cdc25 Phosphatases citation: Wipf, P and Aslan, DC and Southwick, EC and Lazo, JS (2001) Sulfonylated aminothiazoles as new small molecule inhibitors of protein phosphatases. Bioorganic and Medicinal Chemistry Letters, 11 (3). 313 - 317. ISSN 0960-894X document_url: http://d-scholarship-dev.library.pitt.edu/20495/1/licence.txt