Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia.
Jarusiewicz JA, Jeon JY, Connelly MC, Chen Y, Yang L, Baker SD, Guy RK
ACS Omega 2 1985-2009 05/31/2017
Profiling of the kinase-binding capabilities of an aminopyrimidine analogue detected in a cellular screen of the St. Jude small-molecule collection led to the identification of a novel series of FMS-like tyrosine kinase 3 (FLT3) inhibitors. Structure-activity relationship studies led to the development of compounds exhibiting good potency against MV4-11 and MOLM13 acute myelogenous leukemia cells driven by FLT3, regardless of their FLT3 mutation status. In vitro pharmacological profiling demonstrated that compoundFull Text