Source:http://linkedlifedata.com/resource/pubmed/id/21486698
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
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pubmed:dateCreated |
2011-5-2
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pubmed:abstractText |
A series of novel N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential telomerase inhibitors were synthesized. The bioassay tests show that compound 4a exhibited high activity against human gastric cancer cell SGC-7901, liver cancer Hep-G2 and human prostate PC-3 cell lines with IC(50) values of 21.23±0.99, 29.43±0.32 and 30.89±1.07 ?M, respectively. All title compounds were assayed for telomerase inhibition by a modified TRAP assay, the results show that compound 4a can inhibit telomerase with IC(50) value of 4.0±0.32 ?M. Docking simulation was performed to position compound 4a into the telomerase (3DU6) active site to determine the probable binding model.
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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 |
May
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:copyrightInfo |
Copyright © 2011 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2916-20
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pubmed:meshHeading |
pubmed-meshheading:21486698-Antineoplastic Agents,
pubmed-meshheading:21486698-Cell Line,
pubmed-meshheading:21486698-Cell Line, Tumor,
pubmed-meshheading:21486698-Cell Proliferation,
pubmed-meshheading:21486698-Drug Design,
pubmed-meshheading:21486698-Humans,
pubmed-meshheading:21486698-Inhibitory Concentration 50,
pubmed-meshheading:21486698-Models, Molecular,
pubmed-meshheading:21486698-Molecular Structure,
pubmed-meshheading:21486698-Pyrazoles,
pubmed-meshheading:21486698-Telomerase
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pubmed:year |
2011
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pubmed:articleTitle |
Design and synthesis of N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agents.
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pubmed:affiliation |
State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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