Document Detail

Solid-phase synthesis of potential protein tyrosine phosphatase inhibitors via the Ugi four-component condensation.
MedLine Citation:
PMID:  9873558     Owner:  NLM     Status:  MEDLINE    
A library of 108 alpha,alpha-difluoromethylenephosphonic acids was prepared by Ugi four-component condensation using Rink-NH2 resin, 4-[(diethoxyphosphinyl) difluoromethyl]benzoic acid, and a set of 18 aldehydes and 6 isonitriles. Following resin cleavage, the diethylphosphonate esters were hydrolyzed with trimethylsilyl bromide to yield the free acids which were assayed for inhibition of PTP alpha, PTP beta and PTP epsilon.
Z Li; S L Yeo; C J Pallen; A Ganesan
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  8     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  1998 Sep 
Date Detail:
Created Date:  1999-02-02     Completed Date:  1999-02-02     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  2443-6     Citation Subset:  IM    
Institute of Molecular and Cell Biology, National University of Singapore.
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MeSH Terms
Chromatography, High Pressure Liquid
Enzyme Inhibitors / chemical synthesis*
Magnetic Resonance Spectroscopy
Models, Chemical
Phosphonic Acids* / chemistry
Protein Conformation
Protein Tyrosine Phosphatases / antagonists & inhibitors*
Reg. No./Substance:
0/Aldehydes; 0/Enzyme Inhibitors; 0/Iodobenzoates; 0/Nitriles; 0/Phosphonic Acids; EC Tyrosine Phosphatases

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