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Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach.


ABSTRACT: Acute myeloid leukemia (AML) is an aggressive malignancy with only a handful of therapeutic options. About 30% of AML patients harbor mutated FLT3 kinase, and thus, this cancer-driver has become a hotly pursued AML target. Herein we report a new class of FLT3 inhibitors, which potently inhibit the proliferation of acute myeloid leukemia (AML) cells at nanomolar concentrations.

SUBMITTER: Ma X 

PROVIDER: S-EPMC5430396 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature

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Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach.

Ma Xiaochu X   Zhou Jie J   Wang Changhao C   Carter-Cooper Brandon B   Yang Fan F   Larocque Elizabeth E   Fine Jonathan J   Tsuji Genichiro G   Chopra Gaurav G   Lapidus Rena G RG   Sintim Herman O HO  

ACS medicinal chemistry letters 20170414 5


Acute myeloid leukemia (AML) is an aggressive malignancy with only a handful of therapeutic options. About 30% of AML patients harbor mutated FLT3 kinase, and thus, this cancer-driver has become a hotly pursued AML target. Herein we report a new class of FLT3 inhibitors, which potently inhibit the proliferation of acute myeloid leukemia (AML) cells at nanomolar concentrations. ...[more]

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