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Article

Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations.

Bioorganic & medicinal chemistry letters - 15 Nov 2020

Zhang Guo, Zhang Wenqing, Shen Chenjian, Nan Jinshan, Chen Ming, Lai Shusheng, Zhong Jiemin, Li Bolin, Wang Tianqi, Wang Yifei, Yang Shengyong, Li Linli

Abstract excerpt

Herein we report the discovery of 1-(5-(tert-butyl)isoxazol-3-yl)-3- (3-fluorophenyl)urea derivatives as new FLT3 inhibitors that are able to overcome the drug resistance mutations: the secondary D835Y and F691L mutations on the basis of the internal tandem duplications (ITD) mutation of FLT3 (FLT3-ITD/D835Y and FLT3-ITD/F691L, respectively). The most potent compound corresponds to...

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PMID: 32891702
DOI: 10.1016/j.bmcl.2020.127532

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