Article
Structure-based design, synthesis and bioactivity evaluation of macrocyclic inhibitors of mutant isocitrate dehydrogenase 2 (IDH2) displaying activity in acute myeloid leukemia cells.
European journal of medicinal chemistry - 1 Oct 2020
Che Jinxin, Huang Feng, Zhang Mengmeng, Xu Gaoya, Qu Bingxue, Gao Jian, Chen Binhui, Zhang Jianjun, Ying Huazhou, Hu Yongzhou, Hu Xiaobei, Zhou Yubo, Gao Anhui, Li Jia, Dong Xiaowu
Abstract excerpt
The enzymes involved in the metabolic pathways in cancer cells have been demonstrated as important therapeutic targets such as the isocitrate dehydrogenase 2 (IDH2). A series of macrocyclic derivatives was designed based on the marketed IDH2 inhibitor AG-221 by using the conformational restriction strategy. The resulted compounds showed moderate to good inhibitory potential against different IDH2-mutant enzymes....
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