Article
Design, synthesis and biological activity of 3-pyrazine-2-yl-oxazolidin-2-ones as novel, potent and selective inhibitors of mutant isocitrate dehydrogenase 1.
Bioorganic & medicinal chemistry - 15 Dec 2017
Ma Tianfang, Zou Fangxia, Pusch Stefan, Yang Lijun, Zhu Qihua, Xu Yungen, Gu Yueqing, von Deimling Andreas, Zha Xiaoming
Abstract excerpt
Isocitrate dehydrogenases (IDHs) catalyze the oxidative decarboxylation of isocitrate to alpha-ketoglutarate (α-KG) generating carbon dioxide and NADPH/NADH. Evidence suggests that the specific mutations in IDH1 are critical to the growth and reproduction of some tumor cells such as gliomas and acute myeloid leukemia, emerging as an attractive antitumor target. In order to discovery potent new mutant IDH1...
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