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ID: ALA3792292
Journal: Bioorg Med Chem Lett
Title: Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit.
Authors: Nakano H, Hasegawa T, Imamura R, Saito N, Kojima H, Okabe T, Nagano T.
Abstract: A non-selective inhibitor (1) of FMS-like tyrosine kinase-3 (FLT3) was identified by fragment screening and systematically modified to afford a potent and selective inhibitor 26. We confirmed that 26 inhibited the growth of FLT-3-activated human acute myeloid leukemia cell line MV4-11. Our design strategy enabled rapid development of a novel type of FLT3 inhibitor from the hit fragment in the absence of target-structural information.
CiteXplore: 26995531