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Abstract <p>A series of novel quinazoline derivatives containing aromatic hydrazones were synthesized and characterized by <sup>1</sup>H NMR, <sup>13</sup>C NMR, MS, and IR. The antitumor activity of the compounds was tested using A549 and MKN45 cell lines with gefitinib and foretinib as positive control drugs. By combining its unique molecular docking model, the target derivatives were docked with proteins to explore the binding mode and biological activity of the target derivatives on the EGFR/c-Met dual target, and the ADME data of the compounds were ultimately predicted. The final proof shown that (<i>E</i>)-4-[3-({4-[2-(3-chlorobenzylidene)hydrazineyl]-7-methoxyquinazolin-6-yl}oxy)propyl]morpholine and (<i>E</i>)-4-[3-({4-[2-(2,4-dichlorobenzylidene)hydrazineyl]-7-methoxyquinazolin-6-yl}oxy)propyl]morpholine have high drug-like properties and further research value.</p>

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Design, Synthesis, and Biological Activity Study of Antitumor Drugs Containing Aryl Hydrazone Quinazoline

  • 期刊论文

  • 发表日期：

    2025年4月25日

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  • Jurang Li,
  • Zhizhuo Qu,
  • Zhiqiang Cai,
  • Chunmeng Li,
  • Yang Liu,
  • Yingnuo Wang,
  • Weidong Zhang,
  • Lekun Wei,
  • Hongying Ji

摘要

Abstract

A series of novel quinazoline derivatives containing aromatic hydrazones were synthesized and characterized by 1H NMR, 13C NMR, MS, and IR. The antitumor activity of the compounds was tested using A549 and MKN45 cell lines with gefitinib and foretinib as positive control drugs. By combining its unique molecular docking model, the target derivatives were docked with proteins to explore the binding mode and biological activity of the target derivatives on the EGFR/c-Met dual target, and the ADME data of the compounds were ultimately predicted. The final proof shown that (E)-4-[3-({4-[2-(3-chlorobenzylidene)hydrazineyl]-7-methoxyquinazolin-6-yl}oxy)propyl]morpholine and (E)-4-[3-({4-[2-(2,4-dichlorobenzylidene)hydrazineyl]-7-methoxyquinazolin-6-yl}oxy)propyl]morpholine have high drug-like properties and further research value.