Article
Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors.
Bioorganic & medicinal chemistry letters - 1 Dec 2016
Han Mei, Li Shan, Ai Jing, Sheng Rong, Hu Yongzhou, Hu Youhong, Geng Meiyu
Abstract excerpt
A series of novel 4-chloro-benzamides derivatives containing substituted five-membered heteroaryl ring were designed, synthesized and evaluated as RET kinase inhibitors for cancer therapy. Most of compounds exhibited moderate to high potency in ELISA-based kinase assay. In particular, compound I-8 containing 1,2,4-oxadiazole strongly inhibited RET kinase activity both in molecular and cellular level. In turn, I-8...
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