Source:http://linkedlifedata.com/resource/pubmed/id/17287120
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
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pubmed:dateCreated |
2007-3-13
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pubmed:abstractText |
Ethacrynic acid (EA), an alpha,beta-unsaturated carbonyl compound, is a glutathione S-transferase P1-1 (GSTP1-1) inhibitor. Twenty-one novel EA derivatives have been synthesized. The effects of these compounds on GSTP1-1 activity and on the proliferation of human leukemia HL-60 cells have been determined. Compounds with a halogen substitution at the 3'-position of the aromatic ring have greater inhibitory effects on GSTP1-1 activity than those of compounds with a methyl substitution there. Compounds with substitutions at both the 2'- and 3'-positions of the aromatic ring have more antiproliferative ability than those with one substitution at 3'-position. Esterification of the carboxyl group appears to increase the antiproliferative ability.
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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 |
Apr
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pubmed:issn |
0968-0896
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2701-7
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pubmed:meshHeading |
pubmed-meshheading:17287120-Antineoplastic Agents,
pubmed-meshheading:17287120-Cell Line, Tumor,
pubmed-meshheading:17287120-Cell Proliferation,
pubmed-meshheading:17287120-Chromatography, Thin Layer,
pubmed-meshheading:17287120-Enzyme Inhibitors,
pubmed-meshheading:17287120-Ethacrynic Acid,
pubmed-meshheading:17287120-Glutathione S-Transferase pi,
pubmed-meshheading:17287120-HL-60 Cells,
pubmed-meshheading:17287120-Humans,
pubmed-meshheading:17287120-Leukemia,
pubmed-meshheading:17287120-Magnetic Resonance Spectroscopy,
pubmed-meshheading:17287120-Spectrophotometry, Infrared,
pubmed-meshheading:17287120-Spectroscopy, Fourier Transform Infrared,
pubmed-meshheading:17287120-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
The synthesis of alpha,beta-unsaturated carbonyl derivatives with the ability to inhibit both glutathione S-transferase P1-1 activity and the proliferation of leukemia cells.
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pubmed:affiliation |
College of Pharmacy, Shandong University, Ji'nan, Shandong Province 250012, PR China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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