Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors.
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Miyazaki Y, Matsunaga S, Tang J, Maeda Y, Nakano M, Philippe RJ, Shibahara M, Liu W, Sato H, Wang L, Nolte RT
Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors.
Bioorg Med Chem Lett. 2005 May 2;15(9):2203-7.
- PubMed ID
- 15837294 [ View in PubMed]
- Abstract
A novel class of furo[2,3-d]pyrimidines has been discovered as potent dual inhibitors of Tie-2 and VEGFR2 receptor tyrosine kinases (TK) and a diarylurea moiety at 5-position shows remarkably enhanced activity against both enzymes. One of the most active compounds, 4-amino-3-(4-((2-fluoro-5-(trifluoromethyl)phenyl)amino-carbonylamino)phenyl)-2-( 4-methoxyphenyl)furo[2,3-d]pyrimidine (7k) is <3 nM on both TK receptors and the activity is rationalized based on the X-ray crystal structure.