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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 |
2010-8-9
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pubmed:abstractText |
The insulin-like growth factor receptor (IGF-1R) is a receptor tyrosine kinase (RTK) involved in all stages of the development and propagation of breast and other cancers. The inhibition of IGF-1R by small molecules remains a promising strategy to treat cancer. Herein, we explore SAR around previously characterized lead compound (1), which is an aryl-heteroaryl urea (AHU) consisting of 4-aminoquinaldine and a substituted aromatic ring system. A library of novel AHU compounds was prepared based on derivatives of the 4-aminoquinoline heterocycle (including various 2-substituted derivatives, and naphthyridines). The compounds were screened for in vitro inhibitory activity against IGF-1R, and several compounds with improved activity (3-5 microM) were identified. Furthermore, a computational docking study was performed, which identifies a fairly consistent lowest energy mode of binding for the more-active set of inhibitors in this series, while the less-active inhibitors do not adopt a consistent mode of binding.
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pubmed:grant |
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/20643554-11426642,
http://linkedlifedata.com/resource/pubmed/commentcorrection/20643554-11694888,
http://linkedlifedata.com/resource/pubmed/commentcorrection/20643554-11908858,
http://linkedlifedata.com/resource/pubmed/commentcorrection/20643554-12466191,
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http://linkedlifedata.com/resource/pubmed/commentcorrection/20643554-15050914,
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http://linkedlifedata.com/resource/pubmed/commentcorrection/20643554-17317169,
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http://linkedlifedata.com/resource/pubmed/commentcorrection/20643554-18410242,
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http://linkedlifedata.com/resource/pubmed/commentcorrection/20643554-19778024,
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http://linkedlifedata.com/resource/pubmed/commentcorrection/20643554-8402902
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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 |
1464-3391
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pubmed:author |
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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 |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5995-6005
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pubmed:dateRevised |
2011-9-26
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pubmed:meshHeading |
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pubmed:year |
2010
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pubmed:articleTitle |
Synthesis of aryl-heteroaryl ureas (AHUs) based on 4-aminoquinoline and their evaluation against the insulin-like growth factor receptor (IGF-1R).
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pubmed:affiliation |
Department of Chemistry & Biochemistry, San Francisco State University, San Francisco, CA 94132, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, N.I.H., Extramural
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