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<p>Cancer remains the leading cause of human morbidity worldwide. A new series of coumarin-quinazolinedion-coumarin conjugates were synthesized and evaluated for their anticancer activity towards selected human cancer cell lines: T-98G glioblastoma, PC-3 prostate, and MCF-7 breast cancer, and HEK-293 human embryonic kidney, utilizing Doxorubicin as a reference drug. Compounds <b>4</b>, <b>3d</b>, and <b>3b</b> derivatives demonstrated higher cytotoxic activity against all cancer cells at 72 h as compared to the reference drug Doxorubicin. Molecular docking analyses revealed that the synthesized compounds bind to the active sites of the ATPase domain of human DNA topoisomerase IIα and support the experimentally determined anticancer activity.</p>

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Biscoumarin Derivatives Bridged Quinazolinedion: Synthesis, Molecular Docking Study, and Cytotoxic Activities

  • 期刊论文

  • 发表日期：

    2025年3月1日

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  • Gülay Akyüz,
  • Emre Menteşe,
  • Suleyman Ilhan,
  • Mustafa Emirik,
  • Harika Atmaca

摘要

Cancer remains the leading cause of human morbidity worldwide. A new series of coumarin-quinazolinedion-coumarin conjugates were synthesized and evaluated for their anticancer activity towards selected human cancer cell lines: T-98G glioblastoma, PC-3 prostate, and MCF-7 breast cancer, and HEK-293 human embryonic kidney, utilizing Doxorubicin as a reference drug. Compounds 4, 3d, and 3b derivatives demonstrated higher cytotoxic activity against all cancer cells at 72 h as compared to the reference drug Doxorubicin. Molecular docking analyses revealed that the synthesized compounds bind to the active sites of the ATPase domain of human DNA topoisomerase IIα and support the experimentally determined anticancer activity.