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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
23
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pubmed:dateCreated |
2010-11-8
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pubmed:abstractText |
A small library of pyrrolidinesulphonylaryl molecules has been synthesized via an efficient 4-step route, and members evaluated for their ability to inhibit IL-6 signalling. One molecule (6a) was found to have promising activity against IL-6/STAT3 signalling at the low micromolar level, and to selectively inhibit phosphorylation of STAT3 (but not STAT1) in IL-6 stimulated MDA-MB-231 breast cancer and HeLa cell lines. It was also selectively cytostatic in MDA-MB-231 (STAT3-dependent) versus A4 (STAT3-null) cells suggesting STAT3-specific inhibitory properties.
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pubmed:grant |
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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 |
Dec
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AndersonJohnJ,
pubmed-author:AntonowDyeisonD,
pubmed-author:BasuB PikuBP,
pubmed-author:EssexSamanthaS,
pubmed-author:HaiderShozebS,
pubmed-author:HaqueMohammad RMR,
pubmed-author:HasanFyezaF,
pubmed-author:KayeSamantha LSL,
pubmed-author:MorgensternDanielD,
pubmed-author:NeidleStephenS,
pubmed-author:PalmerJonathanJ,
pubmed-author:RahmanKhondaker MKM,
pubmed-author:ThurstonDavid EDE,
pubmed-author:WilderspinAndrew FAF,
pubmed-author:ZinzallaGiovannaG
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pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
7029-32
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pubmed:meshHeading |
pubmed-meshheading:21030257-Breast Neoplasms,
pubmed-meshheading:21030257-Cell Line, Tumor,
pubmed-meshheading:21030257-Cytostatic Agents,
pubmed-meshheading:21030257-Female,
pubmed-meshheading:21030257-HeLa Cells,
pubmed-meshheading:21030257-Humans,
pubmed-meshheading:21030257-Interleukin-6,
pubmed-meshheading:21030257-Phosphorylation,
pubmed-meshheading:21030257-Pyrrolidines,
pubmed-meshheading:21030257-STAT3 Transcription Factor,
pubmed-meshheading:21030257-Signal Transduction,
pubmed-meshheading:21030257-Small Molecule Libraries,
pubmed-meshheading:21030257-Structure-Activity Relationship,
pubmed-meshheading:21030257-Sulfones
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pubmed:year |
2010
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pubmed:articleTitle |
A novel small-molecule inhibitor of IL-6 signalling.
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pubmed:affiliation |
Cancer Research UK Protein, The School of Pharmacy, University of London, London, United Kingdom.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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