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Article

Discovery of a Potent FLT3 Inhibitor (LT-850-166) with the Capacity of Overcoming a Variety of FLT3 Mutations.

Journal of medicinal chemistry - 14 Oct 2021

Wang Zhijie, Cai Jiongheng, Ren Jiwei, Chen Yun, Wu Yingli, Cheng Jie, Jia Kun, Huang Fei, Cheng Zitian, Sheng Tiancheng, Song Shiyu, Heng Hao, Zhu Yifan, Tang Weifang, Li Hongmei, Lu Tao, Chen Yadong, Lu Shuai

Abstract excerpt

Secondary mutations of FLT3 have become the main mechanism of FLT3 inhibitor resistance that presents a significant clinical challenge. Herein, a series of pyrazole-3-amine derivatives were synthesized and optimized to overcome the common secondary resistance mutations of FLT3. The structure-activity relationship and molecular dynamics simulation studies illustrated that the ribose region of FLT3 could be...

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Identifiers

PMID: 34550682
DOI: 10.1021/acs.jmedchem.1c01196

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Discovery of a Potent FLT3 Inhibitor (LT-850-166) with the Capacity of Overcoming a Variety of FLT3 Mutations.PMID 34550682Read ↗

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Design and synthesis 1H-Pyrrolo[2,3-b]pyridine derivatives as FLT3 inhibitors for the treatment of Acute myeloid Leukemia.Semantic proximity Read ↗

N-(3-Methoxyphenyl)-6-(7-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl)pyridin-2-amine is an inhibitor of the FLT3-ITD and BCR-ABL pathways, and potently inhibits FLT3-ITD/D835Y and FLT3-ITD/F691L secondary mutants.Semantic proximity Read ↗

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Rational design of 4-((6-phenoxypyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (LT-540-717) as orally bioavailable FLT3 inhibitor.Semantic proximity Read ↗

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Deciphering the mechanism of HM43239 inhibiting the mutant F691L resistant to gilteritinib in FMS-like tyrosine kinase 3.Semantic proximity Read ↗

Structural Optimization and MD Simulation Study of Benzimidazole Derivatives as Potent Mutant FLT3 Kinase Inhibitors Targeting AMLSemantic proximity Read ↗

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