Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (Volitinib) as a Highly Potent and Selective

详细信息    查看全文

• 作者：Hong Jia ; Guangxiu Dai ; Jianyang Weng ; Zhulin Zhang ; Qing Wang ; Feng Zhou ; Longxian Jiao ; Yumin Cui ; Yongxin Ren ; Shiming Fan ; Jinghong Zhou ; Weiguo Qing ; Yi Gu ; Jian Wang ; Yang Sai ; Weiguo Su
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：September 25, 2014
• 年：2014
• 卷：57
• 期：18
• 页码：7577-7589
• 全文大小：536K
• ISSN：1520-4804

文摘

HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure鈥揳ctivity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.