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Article

Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants.

Journal of medicinal chemistry - 14 Jul 2016

Sun Deheng, Yang Yu, Lyu Jiankun, Zhou Wei, Song Wenlin, Zhao Zhenjiang, Chen Zhuo, Xu Yufang, Li Honglin

Abstract excerpt

FLT3 has been validated as a therapeutic target for the treatment of acute myeloid leukemia (AML). In this paper, we describe for the first time, pteridin-7(8H)-one as a scaffold for potent FLT3 inhibitors derived from structural optimizations on irreversible EGFR inhibitors. The representative inhibitor (31) demonstrates single-digit nanomolar inhibition against FLT3 and subnanomolar KD for drug-resistance FLT3...

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Source

Identifiers

PMID: 27266526
DOI: 10.1021/acs.jmedchem.6b00374

Genes

FLT3
EGFR

Provenance

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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