Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595986 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
A series of novel 5-(benzyloxy)pyridin-2(1H)-ones were designed, synthesized and biologically evaluated for c-Met inhibition. The carbonyl oxygen of the pyridin-2(1H)-one was demonstrated to be an important factor for c-Met binding affinity. Various amides and benzoimidazoles at C-3 position of the pyridin-2(1H)-one core were investigated. A potent compound 12b with a c-Met IC50 of 12Â nM was identified. This compound exhibited potent inhibition of EBC-1 cell associated with c-Met constitutive activation and showed high selectivity for c-Met than other tested 11 kinases.
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Organic Chemistry
Authors
Dengyou Zhang, Jing Ai, Zhongjie Liang, Wei Zhu, Xia Peng, Xianjie Chen, YinChun Ji, Hualiang Jiang, Cheng Luo, Meiyu Geng, Hong Liu,