|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0021469,
umls-concept:C0034284,
umls-concept:C0205177,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0243072,
umls-concept:C0442027,
umls-concept:C0596087,
umls-concept:C1334306,
umls-concept:C1336602,
umls-concept:C1527415,
umls-concept:C1705001
|
|
pubmed:issue |
6
|
|
pubmed:dateCreated |
2007-2-23
|
|
pubmed:abstractText |
During our effort to develop dual VEGFR2 and Tie-2 inhibitors as anti-angiogenic agents for cancer therapy, we discovered 4-amino-5-(4-((2-fluoro-5-(trifluoromethyl)phenyl)- aminocarbonylamino)phenyl)furo[2,3-d]pyrimidine (8a) possessing strong inhibitory activity at both the enzyme and cellular level against VEGFR2 and Tie-2. Compound 8a demonstrated high pharmacokinetic exposure through oral administration, and showed marked tumor growth inhibition and anti-angiogenic activity in mouse HT-29 xenograft model via once-daily oral administration.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Mar
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:HasslerDaniel FDF,
pubmed-author:HoMaureen LML,
pubmed-author:MaedaYutakaY,
pubmed-author:MiyazakiYasushiY,
pubmed-author:NakanoMasatoM,
pubmed-author:NarteyEldridge NEN,
pubmed-author:NolteRobert TRT,
pubmed-author:OkamotoYujiY,
pubmed-author:OzawaKazunoriK,
pubmed-author:PatrickDenis RDR,
pubmed-author:SatoHideyukiH,
pubmed-author:SugaiMasakiM,
pubmed-author:TangJunJ,
pubmed-author:TruesdaleAnne TAT,
pubmed-author:WangLipingL
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
15
|
|
pubmed:volume |
17
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1773-8
|
|
pubmed:dateRevised |
2009-11-19
|
|
pubmed:meshHeading |
pubmed-meshheading:17276055-Angiogenesis Inhibitors,
pubmed-meshheading:17276055-Animals,
pubmed-meshheading:17276055-Antineoplastic Agents,
pubmed-meshheading:17276055-Area Under Curve,
pubmed-meshheading:17276055-Computer Simulation,
pubmed-meshheading:17276055-Crystallography, X-Ray,
pubmed-meshheading:17276055-Drug Evaluation, Preclinical,
pubmed-meshheading:17276055-Female,
pubmed-meshheading:17276055-HT29 Cells,
pubmed-meshheading:17276055-Humans,
pubmed-meshheading:17276055-Indicators and Reagents,
pubmed-meshheading:17276055-Male,
pubmed-meshheading:17276055-Mice,
pubmed-meshheading:17276055-Models, Molecular,
pubmed-meshheading:17276055-Neoplasm Transplantation,
pubmed-meshheading:17276055-Pyrimidines,
pubmed-meshheading:17276055-RNA,
pubmed-meshheading:17276055-Receptor, TIE-2,
pubmed-meshheading:17276055-Urea,
pubmed-meshheading:17276055-Vascular Endothelial Growth Factor Receptor-2
|
|
pubmed:year |
2007
|
|
pubmed:articleTitle |
Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2.
|
|
pubmed:affiliation |
GlaxoSmithKline, Tsukuba Research Laboratories, 43, Wadai, Tsukuba 300-4247, Ibaraki, Japan. yasushi.miyazaki@gsk.com
|
|
pubmed:publicationType |
Journal Article
|
