Document Report Card

Basic Information

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

DOI: 10.1016/j.bmcl.2016.03.006