rdf:type |
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lifeskim:mentions |
|
pubmed:issue |
5-7
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pubmed:dateCreated |
2005-10-26
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pubmed:abstractText |
A combination of mechanism-based and structure-based design strategies led to the synthesis of a series of 5- and 6-substituted uracil derivatives as potential inhibitors of thymidine phosphorlase/platelet derived endothelial cell growth factor (TP/PD-ECGF). Among those tested, 6-imidazolylmethyl-5-fluorouracil was found to be the most potent inhibitor with a Ki-value of 51 nM, representing a new class of 5-fluoropyrimidines with a novel mechanism of action.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
|
pubmed:status |
MEDLINE
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pubmed:issn |
1525-7770
|
pubmed:author |
|
pubmed:issnType |
Print
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pubmed:volume |
24
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
367-73
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pubmed:meshHeading |
pubmed-meshheading:16247953-Binding Sites,
pubmed-meshheading:16247953-Enzyme Inhibitors,
pubmed-meshheading:16247953-Escherichia coli,
pubmed-meshheading:16247953-Fluorouracil,
pubmed-meshheading:16247953-Humans,
pubmed-meshheading:16247953-Imidazoles,
pubmed-meshheading:16247953-Inhibitory Concentration 50,
pubmed-meshheading:16247953-Kinetics,
pubmed-meshheading:16247953-Models, Chemical,
pubmed-meshheading:16247953-Pyrimidines,
pubmed-meshheading:16247953-Thymidine Phosphorylase
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pubmed:year |
2005
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pubmed:articleTitle |
6-substituted 5-fluorouracil derivatives as transition state analogue inhibitors of thymidine phosphorylase.
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pubmed:affiliation |
Department of Chemistry, University at Buffalo, Amherst, NY 14260, USA. tkalman@buffalo.edu
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pubmed:publicationType |
Journal Article
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