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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2010-3-22
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pubmed:abstractText |
A series of 5-ureidobenzofuranones was discovered as potent and selective inhibitors of mTOR with good cellular activity. Molecular modeling studies revealed several hydrogen bond interactions of the ureido group with the enzyme at the ATP-binding site. Furthermore, modeling showed that the ureido group is best situated at C-5 of the benzofuranone. Syntheses of 4-ureido and 5-ureidobenzofuranones are presented.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine Triphosphate,
http://linkedlifedata.com/resource/pubmed/chemical/Benzofurans,
http://linkedlifedata.com/resource/pubmed/chemical/Class Ib Phosphatidylinositol...,
http://linkedlifedata.com/resource/pubmed/chemical/Intracellular Signaling Peptides...,
http://linkedlifedata.com/resource/pubmed/chemical/Isoenzymes,
http://linkedlifedata.com/resource/pubmed/chemical/MTOR protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/PIK3CG protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphatidylinositol 3-Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Protein-Serine-Threonine Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/Sirolimus,
http://linkedlifedata.com/resource/pubmed/chemical/TOR Serine-Threonine Kinases
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:copyrightInfo |
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 |
2259-63
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:20188551-Adenosine Triphosphate,
pubmed-meshheading:20188551-Animals,
pubmed-meshheading:20188551-Benzofurans,
pubmed-meshheading:20188551-Class Ib Phosphatidylinositol 3-Kinase,
pubmed-meshheading:20188551-Crystallography, X-Ray,
pubmed-meshheading:20188551-Humans,
pubmed-meshheading:20188551-Hydrogen Bonding,
pubmed-meshheading:20188551-Intracellular Signaling Peptides and Proteins,
pubmed-meshheading:20188551-Isoenzymes,
pubmed-meshheading:20188551-Models, Molecular,
pubmed-meshheading:20188551-Phosphatidylinositol 3-Kinases,
pubmed-meshheading:20188551-Protein Kinase Inhibitors,
pubmed-meshheading:20188551-Protein-Serine-Threonine Kinases,
pubmed-meshheading:20188551-Sirolimus,
pubmed-meshheading:20188551-Structural Homology, Protein,
pubmed-meshheading:20188551-TOR Serine-Threonine Kinases
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pubmed:year |
2010
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pubmed:articleTitle |
4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
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pubmed:affiliation |
Chemical Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965, United States. tsouh@wyeth.com
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pubmed:publicationType |
Journal Article
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