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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
13
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pubmed:dateCreated |
2006-6-22
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pubmed:abstractText |
Substituted 3-((2-(pyridin-2-ylamino)thiazol-5-ylmethyl)amino)benzamides were identified as potent and selective inhibitors of vascular endothelial growth factor receptor-2 (VEGFR-2) kinase activity. The enzyme kinetics associated with the VEGFR-2 inhibition of 14 (Ki=49+/-9 nM) confirmed that the aminothiazole-based analogues are competitive with ATP. Analogue 14 demonstrated excellent kinase selectivity, favorable pharmacokinetic properties in multiple species, and robust in vivo efficacy in human lung and colon carcinoma xenograft models.
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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 |
Jun
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BarrishJoel CJC,
pubmed-author:BhideRajeev SRS,
pubmed-author:BorzilleriRobert MRM,
pubmed-author:D'ArienzoCelia JCJ,
pubmed-author:DerbinGeorge MGM,
pubmed-author:FargnoliJosephJ,
pubmed-author:HuntJohn TJT,
pubmed-author:JeyaseelanRobertRSr,
pubmed-author:KamathAmritaA,
pubmed-author:KukralDaniel WDW,
pubmed-author:LombardoLouis JLJ,
pubmed-author:MarathePunitP,
pubmed-author:MortilloSteveS,
pubmed-author:QianLigangL,
pubmed-author:TokarskiJohn SJS,
pubmed-author:WautletBarri SBS,
pubmed-author:ZhengXiaopingX
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pubmed:issnType |
Print
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pubmed:day |
29
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pubmed:volume |
49
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3766-9
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:16789733-Administration, Oral,
pubmed-meshheading:16789733-Aminopyridines,
pubmed-meshheading:16789733-Angiogenesis Inhibitors,
pubmed-meshheading:16789733-Animals,
pubmed-meshheading:16789733-Binding Sites,
pubmed-meshheading:16789733-Cell Proliferation,
pubmed-meshheading:16789733-Endothelial Cells,
pubmed-meshheading:16789733-Endothelium, Vascular,
pubmed-meshheading:16789733-Humans,
pubmed-meshheading:16789733-Macaca fascicularis,
pubmed-meshheading:16789733-Mice,
pubmed-meshheading:16789733-Mice, Nude,
pubmed-meshheading:16789733-Models, Molecular,
pubmed-meshheading:16789733-Rats,
pubmed-meshheading:16789733-Structure-Activity Relationship,
pubmed-meshheading:16789733-Thiazoles,
pubmed-meshheading:16789733-Umbilical Veins,
pubmed-meshheading:16789733-Vascular Endothelial Growth Factor Receptor-2,
pubmed-meshheading:16789733-Xenograft Model Antitumor Assays
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pubmed:year |
2006
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pubmed:articleTitle |
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.
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pubmed:affiliation |
Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 4000, Princeton, New Jersey 08543-4000, USA. robert.borzilleri@bms.com
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pubmed:publicationType |
Journal Article,
In Vitro
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