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Article

An imidazo[1,2-a]pyridine-pyridine derivative potently inhibits FLT3-ITD and FLT3-ITD secondary mutants, including gilteritinib-resistant FLT3-ITD/F691L.

European journal of medicinal chemistry - 15 Jan 2024

Wang Xiuqi, DeFilippis Rosa Anna, Weldemichael Tsigereda, Gunaganti Naresh, Tran Phuc, Leung Yuet-Kin, Shah Neil P, Li Hong-Yu

Abstract excerpt

FLT3 activating mutations are detected in approximately 30 % of newly diagnosed acute myeloid leukemia (AML) cases, most commonly consisting of internal tandem duplication (ITD) mutations in the juxtamembrane region. Recently, several FLT3 inhibitors have demonstrated clinical activity and three are currently approved - midostaurin, quizartinib, and gilteritinib. Midostaurin is a first-generation FLT3 inhibitor...

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Identifiers

PMID: 38056299
DOI: 10.1016/j.ejmech.2023.115977
PMCID: PMC11590664

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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An imidazo[1,2-a]pyridine-pyridine derivative potently inhibits FLT3-ITD and FLT3-ITD secondary mutants, including gilteritinib-resistant FLT3-ITD/F691L.PMID 38056299Read ↗

N-(3-Methoxyphenyl)-6-(7-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl)pyridin-2-amine is an inhibitor of the FLT3-ITD and BCR-ABL pathways, and potently inhibits FLT3-ITD/D835Y and FLT3-ITD/F691L secondary mutants.Semantic proximity Read ↗

Discovery of a Potent FLT3 Inhibitor (LT-850-166) with the Capacity of Overcoming a Variety of FLT3 Mutations.Semantic proximity Read ↗

The type I FLT3 inhibitor XL999 overrides secondary FLT3-ITD mutations that arise under gilteritinib and quizartinib treatment in acute myeloid leukemia.Semantic proximity Read ↗

Therapeutic Targeting of FLT3 in Acute Myeloid Leukemia: Current Status and Novel ApproachesSemantic proximity Read ↗

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Gilteritinib is a clinically active FLT3 inhibitor with broad activity against FLT3 kinase domain mutations.Semantic proximity Read ↗

Identification of inhibitors targeting the FLT3-ITD mutation through 4D-QSAR, in vitro, and in silico.Semantic proximity Read ↗

Discovery of indirubin-3'-aminooxy-acetamide derivatives as potent and selective FLT3/D835Y mutant kinase inhibitors for acute myeloid leukemia.Semantic proximity Read ↗

Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations.Semantic proximity Read ↗

Discovery of the selective and efficacious inhibitors of FLT3 mutations.Semantic proximity Read ↗

Discovery of imidazo[1,2-a]pyridine-thiophene derivatives as FLT3 and FLT3 mutants inhibitors for acute myeloid leukemia through structure-based optimization of an NEK2 inhibitor.Semantic proximity Read ↗

The potential of triplet combination therapies for patients with FLT3-ITD -mutated acute myeloid leukemia.Semantic proximity Read ↗

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