Novel 4-amino-furo [2, 3-d] pyrimidines as Tie-2 and VEGFR2 dual inhibitors

Y Miyazaki, S Matsunaga, J Tang, Y Maeda…

Index: Miyazaki, Yasushi; Matsunaga, Shinichiro; Tang, Jun; Maeda, Yutaka; Nakano, Masato; Philippe, Rocher J.; Shibahara, Megumi; Liu, Wei; Sato, Hideyuki; Wang, Liping; Nolte, Robert T. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 9 p. 2203 - 2207

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Citation Number: 119

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< 3nM on both TK receptors and the activity ...