期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 25, 期 12, 页码 3195-3205出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.04.003
关键词
c-Met; Inhibitor; Type II; Pyridine; Pyrimidine; Anti-cancer
资金
- Health care and key specialist scientific research project of Hangzhou Administration of Science and Technology [20140733Q42]
- Major science and technology innovation program of Hangzhou [20142013A60, 20152013A03]
In this study, a series of novel pyridine and pyrimidine-containing derivatives were designed, synthesized and biologically evaluated for their c-Met inhibitory activities. In the biological evaluation, half of the target compounds exhibited moderate to potent c-Met inhibitory activities. Among which, it is noteworthy that compounds 13d not only showed most potent c-Met inhibitory potency but also displayed excellent anti-proliferative activity (IC50 = 127 nM against EBC-1 cell line) as well as an acceptable kinase selectivity profile. Moreover, the western blot assay indicated that 13d inhibited c-Met phosphorylation in EBC-1 cells in a dose-dependent manner, with complete abolishment at 0.1 mM. All these experimental results suggested that 13d could be served as a promising lead compound for the development of anticancer agents. (C) 2017 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据