Article
Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.
Journal of medicinal chemistry - 24 Dec 2015
Li Xixiang, Wang Aoli, Yu Kailin, Qi Ziping, Chen Cheng, Wang Wenchao, Hu Chen, Wu Hong, Wu Jiaxin, Zhao Zheng, Liu Juan, Zou Fengming, Wang Li, Wang Beilei, Wang Wei, Zhang Shanchun, Liu Jing, Liu Qingsong
Abstract excerpt
FLT3-ITD mutant has been observed in about 30% of AML patients and extensively studied as a drug discovery target. On the basis of the structure of PCI-32765 (ibrutinib), a BTK kinase inhibitor that was recently reported to bear FLT3 kinase activity through a structure-guided drug design approach, we have discovered compound 18 (CHMFL-FLT3-122), which displayed an IC50 of 40 nM against FLT3 kinase and achieved...
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