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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
2010-8-19
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pubmed:abstractText |
A series of pyrrole-indolin-2-ones were synthesized, and their inhibition profile for Aurora kinases was studied. The potent compound 33 with phenylsulfonamido at the C-5 position and a carboxyethyl group at the C-3' position selectively inhibited Aurora A over Aurora B with IC50 values of 12 and 156 nM, respectively. Replacement of the carboxyl group with an amino group led to compound 47, which retained the activity for Aurora B and lost activity for Aurora A (IC50=2.19 microM). Computation modeling was used to address the different inhibition profiles of 33 and 47. Compounds 47 and 36 (the ethyl ester analogue of 33) inhibited the proliferation of HCT-116 and HT-29 cells and suppressed levels of the phosphorylated substrates of Aurora A and Aurora B in the Western blots.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:ChangJia-MingJM,
pubmed-author:ChenPaonienP,
pubmed-author:ChiWei-KuangWK,
pubmed-author:ChiangChao-ChengCC,
pubmed-author:ChuangShih-HsienSH,
pubmed-author:HuangHung-JyunHJ,
pubmed-author:HuangJiann-JyhJJ,
pubmed-author:LaiChun-LiangCL,
pubmed-author:LeeYing-ShuenYS,
pubmed-author:LiaoChu-BinCB,
pubmed-author:LinShu FuSF,
pubmed-author:LinYu-HsiangYH,
pubmed-author:LiuChiaweiC,
pubmed-author:TengLi-WeiLW,
pubmed-author:WangRu-WenRW,
pubmed-author:WeiWin-YinWY,
pubmed-author:YangJu-YingJY,
pubmed-author:YangSheng-chuanSC,
pubmed-author:YuanTa-TungTT
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pubmed:issnType |
Electronic
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pubmed:day |
26
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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 |
5929-41
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pubmed:dateRevised |
2011-7-11
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pubmed:meshHeading |
pubmed-meshheading:20681538-Antineoplastic Agents,
pubmed-meshheading:20681538-Cell Proliferation,
pubmed-meshheading:20681538-Drug Screening Assays, Antitumor,
pubmed-meshheading:20681538-HCT116 Cells,
pubmed-meshheading:20681538-HT29 Cells,
pubmed-meshheading:20681538-HeLa Cells,
pubmed-meshheading:20681538-Histones,
pubmed-meshheading:20681538-Humans,
pubmed-meshheading:20681538-Indoles,
pubmed-meshheading:20681538-Models, Molecular,
pubmed-meshheading:20681538-Phosphorylation,
pubmed-meshheading:20681538-Protein Binding,
pubmed-meshheading:20681538-Protein-Serine-Threonine Kinases,
pubmed-meshheading:20681538-Pyrroles,
pubmed-meshheading:20681538-Stereoisomerism,
pubmed-meshheading:20681538-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
Discovery of pyrrole-indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile.
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pubmed:affiliation |
Development Center for Biotechnology, No. 101, Lane 169, Kangning Street, Xizhi City, Taipei County, Taiwan 221, ROC.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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