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Sulfonylated aminothiazoles as new small molecule inhibitors of protein phosphatases

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

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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.


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Item Type: Article
Status: Published
CreatorsEmailPitt UsernameORCID
Wipf, Ppwipf@pitt.eduPWIPF
Aslan, DC
Southwick, EC
Lazo, JS
Date: 12 February 2001
Date Type: Publication
Journal or Publication Title: Bioorganic and Medicinal Chemistry Letters
Volume: 11
Number: 3
Page Range: 313 - 317
DOI or Unique Handle: 10.1016/s0960-894x(00)00658-2
Schools and Programs: Dietrich School of Arts and Sciences > Chemistry
Refereed: Yes
ISSN: 0960-894X
MeSH Headings: Cell Cycle Proteins--antagonists & inhibitors; Combinatorial Chemistry Techniques; Dual Specificity Phosphatase 3; Enzyme Inhibitors--chemical synthesis; Enzyme Inhibitors--pharmacology; Humans; Inhibitory Concentration 50; Phosphoprotein Phosphatases--antagonists & inhibitors; Protein Tyrosine Phosphatase, Non-Receptor Type 1; Protein Tyrosine Phosphatases--antagonists & inhibitors; Structure-Activity Relationship; Sulfonic Acids--chemical synthesis; Sulfonic Acids--pharmacology; Thiazoles--chemical synthesis; Thiazoles--pharmacology; cdc25 Phosphatases--antagonists & inhibitors
PubMed ID: 11212099
Date Deposited: 13 Feb 2014 23:18
Last Modified: 22 Jun 2021 12:55


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