Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia | Zendy

Jamie Jarusiewicz | Zendy; Jae Yoon Jeon | Zendy; Michele Connelly | Zendy; Yizhe Chen | Zendy; Lei Yang | Zendy; Sharyn D. Baker | Zendy; R. Kiplin Guy | Zendy

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Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia

Author(s) -

Jamie Jarusiewicz,

Jae Yoon Jeon,

Michele Connelly,

Yizhe Chen,

Lei Yang,

Sharyn D. Baker,

R. Kiplin Guy

Publication year - 2017

Publication title -

acs omega

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.779

H-Index - 40

ISSN - 2470-1343

DOI - 10.1021/acsomega.7b00144

Subject(s) - myeloid leukemia , cd135 , potency , tyrosine kinase , fms like tyrosine kinase 3 , leukemia , in vitro , kinase , cancer research , tyrosine kinase inhibitor , profiling (computer programming) , drug discovery , pharmacology , chemistry , medicine , signal transduction , mutation , immunology , biochemistry , computer science , cancer , gene , operating system

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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