Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice | Zendy

Nimishetti Naganna | Zendy; Clement OpokuTemeng | Zendy; Eun Yong Choi | Zendy; Elizabeth Larocque | Zendy; Elizabeth Chang | Zendy; Brandon CarterCooper | Zendy; Modi Wang | Zendy; Sandra TorregrosaAllen | Zendy; Bennett D. Elzey | Zendy; Rena G. Lapidus | Zendy; Herman O. Sintim | Zendy

Open Access

Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice

Author(s) -

Nimishetti Naganna,

Clement OpokuTemeng,

Eun Yong Choi,

Elizabeth Larocque,

Elizabeth Chang,

Brandon CarterCooper,

Modi Wang,

Sandra TorregrosaAllen,

Bennett D. Elzey,

Rena G. Lapidus,

Herman O. Sintim

Publication year - 2019

Publication title -

ebiomedicine

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.596

H-Index - 63

ISSN - 2352-3964

DOI - 10.1016/j.ebiom.2019.01.012

Subject(s) - myeloid leukemia , cancer research , tyrosine kinase , in vivo , leukemia , fms like tyrosine kinase 3 , medicine , pharmacology , ex vivo , myeloid , chemistry , mutation , biology , receptor , biochemistry , gene , microbiology and biotechnology

Acute myeloid leukemia (AML) remains one of the most lethal, rarely cured cancers, despite decades of active development of AML therapeutics. Currently, the 5-year survival of AML patients is about 30% and for elderly patients, the rate drops to <10%. About 30% of AML patients harbor an activating mutation in the tyrosine kinase domain (TKD) of Fms-Like Tyrosine kinase 3 (FLT3) or a FLT3 internal tandem duplication (FLT3-ITD). Inhibitors of FLT3, such as Rydapt that was recently approved by the FDA, have shown good initial response but patients often relapse due to secondary mutations in the FLT3 TKD, like D835Y and F691 L mutations.

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