Development of pyridazinone derivatives linked ethyl-bridged-1,2,4-triazole for potential cancer therapy

Merde İ. B., Aykaç O., Hepokur C., Yaşa Y. Z., Taşkor Önel G., Türkmenoğlu B.

Journal of Molecular Structure, cilt.1349, 2026 (SCI-Expanded, Scopus) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 1349
  • Basım Tarihi: 2026
  • Doi Numarası: 10.1016/j.molstruc.2025.143827
  • Dergi Adı: Journal of Molecular Structure
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Chemical Abstracts Core, Chimica, Compendex, INSPEC
  • Anahtar Kelimeler: Anticancer activity, Molecular docking, Pyridazinone derivatives, Triazole
  • Erzincan Binali Yıldırım Üniversitesi Adresli: Evet

Özet

A series of novel pyridazinone derivatives linked ethyl-bridged-1,2,4-triazole were synthesized starting from p-chloroacetophenone. The chemical structures of the compounds 5(a-f) were identified by 1HNMR, 13CNMR and LC-QTOF-MS analysis. In this study, the DDPH method was used to evaluate the antioxidant properties of the compounds. The anticancer activity of the compounds was investigated by MTT method in MCF-7, MDA-MB-231 and L929 cell lines. Gene expression levels of Bcl2, Bax and Casp9 genes were compared, and stages of cell death were determined with high accuracy by flow cytometry. Since compound 5a showed promising cytotoxic effects, molecular docking study was performed to support these results and binding values against Bcl2 anti-apoptotic (PDB ID: 6QGG), Bcl-2 (PDB ID: 4IEH) and tubulin regulation (PDB ID: 1SA0) targets were calculated.