Orally active 4-amino-5-diarylurea-furo [2, 3-d] pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2

…, M Sugai, Y Okamoto, AT Truesdale, DF Hassler…

文献索引：Miyazaki, Yasushi; Tang, Jun; Maeda, Yutaka; Nakano, Masato; Wang, Liping; Nolte, Robert T.; Sato, Hideyuki; Sugai, Masaki; Okamoto, Yuji; Truesdale, Anne T.; Hassler, Daniel F.; Nartey, Eldridge N.; Patrick, Denis R.; Ho, Maureen L.; Ozawa, Kazunori Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 6 p. 1773 - 1778 Title/Abstract Full Text View citing articles Show Details Miyazaki, Yasushi; Maeda, Yutaka; Sato, Hideyuki; Nakano, Masato; Mellor, Geoffrey W. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 6 p. 1967 - 1971

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被引用次数: 33

摘要

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 ...