Source:http://linkedlifedata.com/resource/pubmed/id/20055416
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Predicate | Object |
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rdf:type | |
lifeskim:mentions |
umls-concept:C0014963,
umls-concept:C0017837,
umls-concept:C0021469,
umls-concept:C0038477,
umls-concept:C0205314,
umls-concept:C0220781,
umls-concept:C0243071,
umls-concept:C0334227,
umls-concept:C0441655,
umls-concept:C0596290,
umls-concept:C0679622,
umls-concept:C1441547,
umls-concept:C1707689,
umls-concept:C1883254
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pubmed:issue |
3
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pubmed:dateCreated |
2010-2-4
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pubmed:abstractText |
Ethacrynic acid (EA) is a glutathione S-transferase P1-1 (GST P1-1) inhibitor with weak antiproliferative ability in tumor cells. By use of the principle of bioisosterism, a series of novel EA oxadiazole analogues were designed and synthesized. The structure-activity relationships of inhibiting GST P1-1 activity and cell proliferation of those EA analogues were investigated in human leukemia HL-60 cells. Our data revealed that those EA oxadiazole analogues had improved antiproliferative activity and most of them had similar or better inhibitory effects on GST P1-1 activity than EA. Compound 6u was one of the potent antiproliferative agents without inhibition of GST P1-1 activity. Compounds 6r and 6s were two potent cell growth inhibitors in several solid tumor cell lines with the concentrations inhibiting half of cell growth of less than 5 microM. Our data suggest that these EA oxadiazole analogues are promising antitumor agents that may act through GST P1-1 inhibition-dependent and/or -independent pathways.
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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 |
Feb
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pubmed:issn |
1520-4804
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
11
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pubmed:volume |
53
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1015-22
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pubmed:meshHeading |
pubmed-meshheading:20055416-Antineoplastic Agents,
pubmed-meshheading:20055416-Cell Proliferation,
pubmed-meshheading:20055416-Ethacrynic Acid,
pubmed-meshheading:20055416-Glutathione S-Transferase pi,
pubmed-meshheading:20055416-Humans,
pubmed-meshheading:20055416-Molecular Structure,
pubmed-meshheading:20055416-Neoplasms,
pubmed-meshheading:20055416-Oxadiazoles,
pubmed-meshheading:20055416-Structure-Activity Relationship,
pubmed-meshheading:20055416-Tumor Cells, Cultured
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pubmed:year |
2010
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pubmed:articleTitle |
Novel oxadiazole analogues derived from ethacrynic acid: design, synthesis, and structure-activity relationships in inhibiting the activity of glutathione S-transferase P1-1 and cancer cell proliferation.
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pubmed:affiliation |
School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, PR China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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