Article
Discovery of 2-Aminopyrimidine Derivatives as Potent Dual FLT3/CHK1 Inhibitors with Significantly Reduced hERG Inhibitory Activities.
Journal of medicinal chemistry - 14 Sept 2023
Li Xuemei, Wang Peipei, Wang Chang, Jin Tingting, Xu Ran, Tong Lexian, Hu Xiaobei, Shen Liteng, Li Jia, Zhou Yubo, Liu Tao
Abstract excerpt
FLT3 inhibitors as single agents have limited effects because of acquired and adaptive resistance and the cardiotoxicity related to human ether-a-go-go-related gene (hERG) channel blockade further impedes safe drugs to the market. Inhibitors having potential to overcome resistance and reduce hERG affinity are highly demanded. Here, we reported a dual FLT3/CHK1 inhibitor 18, which displayed potencies to overcome...
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