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Discovery of a novel class of pyridine derivatives that selectively inhibits mutant isocitrate dehydrogenase 2.

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机构： [1]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu, China [2]Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu, China [3]Hinova Pharmaceuticals Inc., Chengdu, China

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关键词： enzyme-based assay IDH IDH2 R140Q mutation pyridine derivatives SAR study

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This paper presents synthesis and structure-activity relationship of pyridine derivatives as inhibitors of mutant isocitrate dehydrogenase 2 (IDH2). A series of 2,4,6-trisubstituted pyridine derivatives have been prepared and evaluated in vitro. Among these compounds, 14n exhibited excellent inhibition activity with the IC50 of 54.6 nm, which is approximately onefold improvement compared to drug candidate AG-221 (Enasidenib) that is in Phase III trial. Exquisite selectivity of 14n for IDH2 R140Q mutant isoform was demonstrated by the poor activity against the wild-type IDH1 and IDH2. © 2017 John Wiley & Sons A/S.

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出版当年[2018]版：

大类 | 3 区医学

小类 | 3 区药物化学 4 区生化与分子生物学

最新[2023]版：

大类 | 4 区医学

小类 | 4 区生化与分子生物学 4 区药物化学

第一作者：

第一作者机构： [1]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu, China

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通讯作者：

通讯机构： [1]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu, China [2]Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu, China [3]Hinova Pharmaceuticals Inc., Chengdu, China [*1]Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu, China. [*2]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu, China.

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