TY - JOUR
T1 - Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia
AU - Jarusiewicz, Jamie A.
AU - Jeon, Jae Yoon
AU - Connelly, Michele C.
AU - Chen, Yizhe
AU - Yang, Lei
AU - Baker, Sharyn D.
AU - Guy, R. Kiplin
N1 - Publisher Copyright:
© 2017 American Chemical Society.
PY - 2017/5/31
Y1 - 2017/5/31
N2 - 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.
AB - 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.
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U2 - 10.1021/acsomega.7b00144
DO - 10.1021/acsomega.7b00144
M3 - Article
AN - SCOPUS:85028978080
VL - 2
SP - 1985
EP - 2009
JO - ACS Omega
JF - ACS Omega
IS - 5
ER -