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Article

Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship.

European journal of medicinal chemistry - 5 Sept 2018

Zhang Ning, Yu Zhimei, Yang Xiaohong, Zhou Yan, Tang Qing, Hu Ping, Wang Jia, Zhang Shao-Lin, Wang Ming-Wei, He Yun

Abstract excerpt

Phosphatidylinositol 3-kinase α (PI3Kα) is the most frequently mutated kinase in human cancers, making it an attractive therapeutic target for cancer treatment. We identified a structurally novel PI3Kα H1047R mutant inhibitor Hit-01 (EC50 = 76.0 μM) through a high-throughput screening campaign. Chemical optimizations enabled us to discover compound 7b, which strongly inhibited PI3Kα H1047R mutant with an EC50...

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PMID: 30071408
DOI: 10.1016/j.ejmech.2018.07.061

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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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