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Article

Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant.

Bioorganic & medicinal chemistry letters - 1 Sept 2015

Lu Xiaoyun, Zhang Zhang, Ren Xiaomei, Pan Xiaofeng, Wang Deping, Zhuang Xiaoxi, Luo Jingfeng, Yu Rongmin, Ding Ke

Abstract excerpt

A series of pyrimidine alkynyl derivatives were designed and synthesized as new Bcr-Abl inhibitors by hybriding the structural moieties from GNF-7, ponatinib and nilotinib. One of the most potent compounds 4e strongly suppresses Bcr-Abl(WT) and Bcr-Abl(T315I) kinase with IC50 values of 5.0 and 9.0 nM, and inhibits the proliferation of K562 and murine Ba/F3 cells ectopically expressing Bcr-Abl(T315I) cells with...

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Identifiers

PMID: 26195136
DOI: 10.1016/j.bmcl.2015.07.006

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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