Article
Discovery of the selective and efficacious inhibitors of FLT3 mutations.
European journal of medicinal chemistry - 15 Jul 2018
Zhi Yanle, Li Baoquan, Yao Chao, Li Hongmei, Chen Puzhou, Bao Jiyin, Qin Tianren, Wang Yue, Lu Tao, Lu Shuai
Abstract excerpt
Fms-like tyrosine kinase 3 (FLT3) is among the most frequently mutated protein in acute myeloid leukemia (AML), which has been confirmed as an important drug target for AML chemotherapy. Starting from the lead compound LT-106-175, a series of 1-H-pyrazole-3-carboxamide derivatives were synthesized to improve the FLT3 inhibitory potency and selectivity. Among them, compound 50 was identified as a highly potent and...
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