Abstract
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 compound 5e shows characteristics suitable for further preclinical development.
Original language | English |
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Pages (from-to) | 1985-2009 |
Number of pages | 25 |
Journal | ACS Omega |
Volume | 2 |
Issue number | 5 |
DOIs | |
State | Published - May 31 2017 |
Bibliographical note
Funding Information:This work was supported by the Department of Defense (CA093469P2), NCI (CA138744-07), St. Jude Children’s Research Hospital, and the American Lebanese Syrian Associated Charities (ALSAC).
Publisher Copyright:
© 2017 American Chemical Society.
ASJC Scopus subject areas
- Chemistry (all)
- Chemical Engineering (all)