Synthesis and biological evaluation of 4-(4-aminophenyl)-6-methylisoxazolo[3,4-b] pyridin-3-amine covalent inhibitors as potential agents for the treatment of acute myeloid leukemia.

doi:10.1016/j.bmc.2022.116937

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Synthesis and biological evaluation of 4-(4-aminophenyl)-6-methylisoxazolo[3,4-b] pyridin-3-amine covalent inhibitors as potential agents for the treatment of acute myeloid leukemia.

Bioorganic & medicinal chemistry - 15 Sept 2022

Kang Ji-Bo, Chen Lu, Leng Xue-Jiao, Wang Jing-Jing, Cheng Yang, Wu Shi-Han, Ma Yi-Yuan, Yang Li-Jin, Cao Yu-Hao, Yang Xiao, Tong Zhen-Jiang, Wu Jia-Zhen, Wang Yi-Bo, Zhou Hai, Liu Jia-Chuan, Ding Ning, Dai Wei-Chen, Yu Yan-Cheng, Xue Xin, Sun Shan-Liang, Dai Xiao-Bin, Chang Liang, Wang Xiao-Long, Li Nian-Guang, Shi Zhi-Hao

Abstract excerpt

Fms-like tyrosine kinase 3 (FLT3) mutation has been strongly associated with increased risk of relapse, and the irreversible covalent FLT3 inhibitors had the potential to overcome the drug-resistance. In this study, a series of simplified 4-(4-aminophenyl)-6-methylisoxazolo[3,4-b] pyridin-3-amine derivatives containing two types of Michael acceptors (vinyl sulfonamide, acrylamide) were conveniently synthesized to...

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PMID: 35863236
DOI: 10.1016/j.bmc.2022.116937

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