501696-52-2Relevant academic research and scientific papers
Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2
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
, p. 1773 - 1778 (2007)
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.
Rational design of 4-amino-5,6-diaryl-furo[2,3-d]pyrimidines as potent glycogen synthase kinase-3 inhibitors
Miyazaki, Yasushi,Maeda, Yutaka,Sato, Hideyuki,Nakano, Masato,Mellor, Geoffrey W.
, p. 1967 - 1971 (2008/12/22)
4-Amino-5,6-diaryl-furo[2,3-d]pyrimidines have been identified as inhibitors of glycogen synthase kinase-3β (GSK-3β). One representative derivative, 4-amino-3-(4-(benzenesulfonylamino)-phenyl)-2-(3-pyridyl)-furo[2,3-d]pyr imidine (12) exhibited potent GSK-3β inhibitory activity in low nanomolar level of IC50. The binding mode was proposed from a docking study.
