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Article

Design and synthesis of novel 2-arylbenzimidazoles as selective mutant isocitrate dehydrogenase 2 R140Q inhibitors.

Bioorganic & medicinal chemistry letters - 1 May 2020

Li Zhenyu, Wu Xingkang, Jia Lejiao, Li Jun, Zhang Rui, Tang Hui, Li Zhiying, Bu Huagang, Shen Chengwu

Abstract excerpt

A series of novel 2-arylbenzimidazoles have been designed, synthesized and evaluated for their inhibitory activity against IDH2 R140Q mutant. The preliminary results indicated that four compounds 7b, 7c, 7m and 7r displayed the potent inhibitory activity against IDH2 R140Q mutant. Among them, compound 7c showed the highest inhibitory activity, with the IC50 value of 0.26 μM, which was more active than positive...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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PMID: 32143887
DOI: 10.1016/j.bmcl.2020.127070

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