Synthesis, characterization, antioxidant and anticancer activity of new hybrid structures based on diarylmethanol and 1,2,3-triazole


Çot A., Betül Özgeriş F. B., Şahin İ., Çeşme M., Onur S., Tümer F.

JOURNAL OF MOLECULAR STRUCTURE, cilt.1269, 2022 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 1269
  • Basım Tarihi: 2022
  • Doi Numarası: 10.1016/j.molstruc.2022.133763
  • Dergi Adı: JOURNAL OF MOLECULAR STRUCTURE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Chemical Abstracts Core, INSPEC
  • Anahtar Kelimeler: Diarylmethanol, 1.2.3-triazole, Antioxidant, Anticancer, Hybrid drug, Molecular docking, TRIAZOLE, DESIGN
  • Atatürk Üniversitesi Adresli: Evet

Özet

Currently, there are many types of cancer, and the search for new anticancer drugs for these types is ongoing. New agents, such as natural compounds, small organic molecules, are being tested for their killing power against these cancer cells due to their anticancer activity. Promising results obtained in hybrid structures containing different pharmacophore units with known activities have made these structures popular. In the presented study, a number of new hybrid structures containing diarylmethanol and 1,2,3triazole units were synthesized. The newly synthesized compounds were structurally analyzed using H-1 NMR, C-13 NMR, elemental analysis and FTIR. The antioxidant and in vitro anticancer activities of all compounds were investigated. It has been determined that the new hybrid structures have very good antioxidant and anticancer activities according to the standards. In particular, compounds 6b, 6h, 6i and 6j (IC50 : 1.87, 12.5 7.22, 8.04 mu g/mL) showed excellent in vitro anticancer activity compared to standard 5-Fu (IC50 : 40.89 mu g/mL). The molecular docking results showed that compounds 6e and 6i have a high affinity by exposed polar and apolar contacts with fundamental residues in the binding pocket of MetAP-2. (c) 2022 Elsevier B.V. All rights reserved.