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rdf:type |
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lifeskim:mentions |
umls-concept:C0044602,
umls-concept:C0205314,
umls-concept:C0220781,
umls-concept:C0243077,
umls-concept:C0285761,
umls-concept:C0439064,
umls-concept:C0679622,
umls-concept:C1150481,
umls-concept:C1368105,
umls-concept:C1451005,
umls-concept:C1521840,
umls-concept:C1527178,
umls-concept:C1704259,
umls-concept:C1705325,
umls-concept:C1705938,
umls-concept:C1705987,
umls-concept:C1707689,
umls-concept:C1883254
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pubmed:issue |
12
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pubmed:dateCreated |
2008-6-10
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pubmed:abstractText |
We herein report the design and synthesis of furoquinoline based novel molecules (16-36) and their in vitro multiple targeted inhibitory potency against PI3K/Akt phosphorylation and mTOR using cell based and cell-free kinase assay. In particular, compound 23 in addition to PI3K-mTOR inhibitory potency, it has shown potent inhibition of hypoxia-induced accumulation of HIF-1alpha protein in U251-HRE cell line. The inhibitory activities of compound 23 were confirmed by Western blot analysis, using human non-small cell lung carcinoma H-460 cell line and glioblastoma U251 cell lines.
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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/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Furans,
http://linkedlifedata.com/resource/pubmed/chemical/Hypoxia-Inducible Factor 1, alpha...,
http://linkedlifedata.com/resource/pubmed/chemical/MTOR protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphatidylinositol 3-Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/Proto-Oncogene Proteins c-akt,
http://linkedlifedata.com/resource/pubmed/chemical/Quinolines,
http://linkedlifedata.com/resource/pubmed/chemical/TOR Serine-Threonine Kinases
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BhatiaDimpleD,
pubmed-author:BhondeMandarM,
pubmed-author:DeoreVijaykumarV,
pubmed-author:KalpanaJoshiJ,
pubmed-author:KumarSanjayS,
pubmed-author:LoharManoj VMV,
pubmed-author:MundadaRamswaroopR,
pubmed-author:PadgaonkarAmolA,
pubmed-author:RathosMaggieM,
pubmed-author:VishwakarmaRam ARA,
pubmed-author:YewalkarNilambariN
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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 |
3603-6
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:18501601-Blotting, Western,
pubmed-meshheading:18501601-Cell Line, Tumor,
pubmed-meshheading:18501601-Drug Design,
pubmed-meshheading:18501601-Enzyme Inhibitors,
pubmed-meshheading:18501601-Furans,
pubmed-meshheading:18501601-Humans,
pubmed-meshheading:18501601-Hypoxia-Inducible Factor 1, alpha Subunit,
pubmed-meshheading:18501601-Molecular Structure,
pubmed-meshheading:18501601-Phosphatidylinositol 3-Kinases,
pubmed-meshheading:18501601-Phosphorylation,
pubmed-meshheading:18501601-Protein Kinases,
pubmed-meshheading:18501601-Proto-Oncogene Proteins c-akt,
pubmed-meshheading:18501601-Quinolines,
pubmed-meshheading:18501601-Signal Transduction,
pubmed-meshheading:18501601-Stereoisomerism,
pubmed-meshheading:18501601-Structure-Activity Relationship,
pubmed-meshheading:18501601-TOR Serine-Threonine Kinases
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pubmed:year |
2008
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pubmed:articleTitle |
Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway.
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pubmed:affiliation |
Department of Medicinal Chemistry, Nicholas Piramal Research Centre, Goregaon (East), Mumbai 400 063, India.
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pubmed:publicationType |
Journal Article
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