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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2008-3-17
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pubmed:abstractText |
A new class of 1-acetanilide-4-aminopyrazole-substituted quinazoline Aurora kinase inhibitors has been discovered possessing highly potent cellular activity. Continuous infusion into athymic mice bearing SW620 tumors of the soluble phosphate derivative 2 led to dose-proportional exposure of the des-phosphate compound 8 with a high-unbound fraction. The combination of potent cell activity and high free-drug exposure led to pharmacodynamic changes in the tumor at low doses, indicative of Aurora B-kinase inhibition and a reduction in tumor volume.
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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/CYP3A4 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Cytochrome P-450 CYP3A,
http://linkedlifedata.com/resource/pubmed/chemical/Ether-A-Go-Go Potassium Channels,
http://linkedlifedata.com/resource/pubmed/chemical/Histones,
http://linkedlifedata.com/resource/pubmed/chemical/KCNH1 protein, human,
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/Pyrazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Quinazolines,
http://linkedlifedata.com/resource/pubmed/chemical/aurora kinase
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BradyMadeleine CMC,
pubmed-author:FooteKevin MKM,
pubmed-author:GreenStephenS,
pubmed-author:HeatonSimon PSP,
pubmed-author:HeronNicola MNM,
pubmed-author:HillGeorge BGB,
pubmed-author:JungFrédéric HFH,
pubmed-author:KearneySarahS,
pubmed-author:KeenNicholas JNJ,
pubmed-author:MortlockAndrew AAA,
pubmed-author:OdedraRajeshR,
pubmed-author:PasquetGeorgesG,
pubmed-author:WedgeStephen RSR,
pubmed-author:WilkinsonRobert WRW
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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 |
1904-9
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pubmed:dateRevised |
2011-7-11
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pubmed:meshHeading |
pubmed-meshheading:18294849-Animals,
pubmed-meshheading:18294849-Cell Cycle,
pubmed-meshheading:18294849-Colonic Neoplasms,
pubmed-meshheading:18294849-Cytochrome P-450 CYP3A,
pubmed-meshheading:18294849-Electrophysiology,
pubmed-meshheading:18294849-Ether-A-Go-Go Potassium Channels,
pubmed-meshheading:18294849-Histones,
pubmed-meshheading:18294849-Humans,
pubmed-meshheading:18294849-Male,
pubmed-meshheading:18294849-Mice,
pubmed-meshheading:18294849-Mice, Nude,
pubmed-meshheading:18294849-Molecular Structure,
pubmed-meshheading:18294849-Phosphorylation,
pubmed-meshheading:18294849-Protein Kinase Inhibitors,
pubmed-meshheading:18294849-Protein-Serine-Threonine Kinases,
pubmed-meshheading:18294849-Pyrazoles,
pubmed-meshheading:18294849-Quinazolines,
pubmed-meshheading:18294849-Rats,
pubmed-meshheading:18294849-Rats, Wistar,
pubmed-meshheading:18294849-Structure-Activity Relationship,
pubmed-meshheading:18294849-Tumor Cells, Cultured,
pubmed-meshheading:18294849-Xenograft Model Antitumor Assays
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pubmed:year |
2008
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pubmed:articleTitle |
Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.
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pubmed:affiliation |
AstraZeneca Pharmaceuticals, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom. kevin.foote@astrazeneca.com
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pubmed:publicationType |
Journal Article
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