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rdf:type |
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lifeskim:mentions |
umls-concept:C0028621,
umls-concept:C0031679,
umls-concept:C0034693,
umls-concept:C0034721,
umls-concept:C0040083,
umls-concept:C0079772,
umls-concept:C0243077,
umls-concept:C0678594,
umls-concept:C1521761,
umls-concept:C1554080,
umls-concept:C1706198,
umls-concept:C1880355,
umls-concept:C1880371
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pubmed:issue |
3
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
Structurally diverse, sugar-modified, thymine-containing nucleoside phosphonic acids were evaluated for their ability to inhibit thymidine phosphorylase (TP, EC 2.4.2.4) purified from spontaneous T-cell lymphomas of an inbred Sprague-Dawley rat strain. From a large set of tested compounds, among them a number of pyrrolidine-based derivatives, 10 nucleotide analogues with IC(50) values below 1 microM were selected. Out of them, four compounds strongly inhibited the enzyme with IC(50) values lying in a range of 11-45 nM. These most potent compounds might be bi-substrate analogues.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BudesínskýMilosM,
pubmed-author:KocalkaPetrP,
pubmed-author:KrálíkováSárkaS,
pubmed-author:LiboskaRadekR,
pubmed-author:PávOndrejO,
pubmed-author:PanovaNatalyaN,
pubmed-author:PetrováMagdalenaM,
pubmed-author:PohlRadekR,
pubmed-author:RejmanDominikD,
pubmed-author:RinnováMarkétaM,
pubmed-author:RosenbergIvanI,
pubmed-author:TocíkZdenekZ,
pubmed-author:TomeckováIvanaI,
pubmed-author:VanekVáclavV,
pubmed-author:VotrubaIvanI
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pubmed:copyrightInfo |
Copyright (c) 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
|
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pubmed:owner |
NLM
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|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
862-5
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pubmed:meshHeading |
pubmed-meshheading:20053558-Animals,
pubmed-meshheading:20053558-Dose-Response Relationship, Drug,
pubmed-meshheading:20053558-Humans,
pubmed-meshheading:20053558-Inhibitory Concentration 50,
pubmed-meshheading:20053558-Lymphoma, T-Cell,
pubmed-meshheading:20053558-Nucleosides,
pubmed-meshheading:20053558-Phosphonic Acids,
pubmed-meshheading:20053558-Rats,
pubmed-meshheading:20053558-Rats, Sprague-Dawley,
pubmed-meshheading:20053558-Structure-Activity Relationship,
pubmed-meshheading:20053558-Thymidine Phosphorylase
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pubmed:year |
2010
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pubmed:articleTitle |
Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase.
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pubmed:affiliation |
Institute of Organic Chemistry and Biochemistry, Academy of Sciences vvi, Flemingovo 2, 166 10 Prague 6, Czech Republic.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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