Source:http://linkedlifedata.com/resource/pubmed/id/20675132
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rdf:type | |
lifeskim:mentions |
umls-concept:C0002072,
umls-concept:C0026029,
umls-concept:C0034693,
umls-concept:C0034721,
umls-concept:C0205070,
umls-concept:C0205198,
umls-concept:C0205474,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0243072,
umls-concept:C0243077,
umls-concept:C0405581,
umls-concept:C1441547,
umls-concept:C1514721,
umls-concept:C1883254
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pubmed:issue |
17
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pubmed:dateCreated |
2010-8-16
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pubmed:abstractText |
We report the synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of (4-substituted phenyl)sulfonate derivatives of 4-hydroxybenzyl imidazole against the two components of 17alpha-hydroxylase/17,20-lyase (P450(17alpha)), namely, 17alpha-hydroxylase (17alpha-OHase) and 17,20-lyase (lyase). The results show the compounds to be highly potent inhibitors with limited selectivity towards the lyase component [e.g., toluene-4-sulfonic acid 4-imidazol-1-ylmethyl-phenyl ester (4) possessed an IC(50) value of 40 nM against 17alpha-OHase and 30 nM against lyase].
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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:month |
Sep
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:copyrightInfo |
Copyright 2010 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 |
5345-8
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pubmed:meshHeading |
pubmed-meshheading:20675132-Animals,
pubmed-meshheading:20675132-Enzyme Inhibitors,
pubmed-meshheading:20675132-Imidazoles,
pubmed-meshheading:20675132-Inhibitory Concentration 50,
pubmed-meshheading:20675132-Male,
pubmed-meshheading:20675132-Microsomes,
pubmed-meshheading:20675132-Models, Molecular,
pubmed-meshheading:20675132-Rats,
pubmed-meshheading:20675132-Steroid 17-alpha-Hydroxylase,
pubmed-meshheading:20675132-Testis
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pubmed:year |
2010
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pubmed:articleTitle |
Synthesis and biochemical evaluation of a range of (4-substituted phenyl)sulfonate derivatives of 4-hydroxybenzyl imidazole-based compounds as potent inhibitors of 17alpha-hydroxylase/17,20-lyase (P45017alpha) derived from rat testicular microsomes.
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pubmed:affiliation |
School of Science, Faculty of Science and Technology, University of the West of Scotland, Paisley, Scotland, UK.
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pubmed:publicationType |
Journal Article
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