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pubmed-article:21486698pubmed:abstractTextA 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.lld:pubmed
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pubmed-article:21486698pubmed:authorpubmed-author:LiuJing-XinJXlld:pubmed
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pubmed-article:21486698pubmed:copyrightInfoCopyright © 2011 Elsevier Ltd. All rights reserved.lld:pubmed
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pubmed-article:21486698pubmed:articleTitleDesign and synthesis of N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agents.lld:pubmed
pubmed-article:21486698pubmed:affiliationState Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China.lld:pubmed
pubmed-article:21486698pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:21486698pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
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