BISCOUMARIN DERIVATIVES BRIDGED QUINAZOLINEDION: SYNTHESIS, MOLECULAR DOCKING STUDY, AND CYTOTOXIC ACTIVITIES

Creative Commons License

Akyüz G., Menteşe E., İlhan M. S., Emirik M., Atmaca H.

PHARMACEUTICAL CHEMISTRY JOURNAL, cilt.58, sa.12, ss.1830-1837, 2025 (SCI-Expanded)

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 58 Sayı: 12
  • Basım Tarihi: 2025
  • Dergi Adı: PHARMACEUTICAL CHEMISTRY JOURNAL
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, BIOSIS, Biotechnology Research Abstracts, Chemical Abstracts Core
  • Sayfa Sayıları: ss.1830-1837
  • Recep Tayyip Erdoğan Üniversitesi Adresli: Evet

Özet

 Cancer remains the leading cause of human morbidity worldwide. A new series of coumarin-quinazoline dion-coumarin conjugates were synthesized and evaluated for their anticancer activity towards selected hu man 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 demon strated 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 DNAtopoisomerase II and support the experimentally determined anticancer activity.