Design, synthesis, and biological evaluation of platinum(II) complexes bearing chiral 2-(1-hydroxyethyl)benzimidazole ligands as potential anticancer agents


Gözelle M., Güler E. M.

POLYHEDRON, cilt.296, 2026 (SCI-Expanded, Scopus) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 296
  • Basım Tarihi: 2026
  • Doi Numarası: 10.1016/j.poly.2026.118228
  • Dergi Adı: POLYHEDRON
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Chemical Abstracts Core, Chimica, Compendex, Academic Search Ultimate (EBSCO), Engineering Source (EBSCO)
  • Gazi Üniversitesi Adresli: Evet

Özet

In this study, a series of novel platinum(II) complexes incorporating chiral 2-(1-hydroxyethyl)benzimidazole ligands was synthesized and characterized. The compounds were evaluated for their cytotoxic activity against three human cancer cell lines, LoVo (human colon adenocarcinoma), HepG2 (human hepatocellular carcinoma), and U87 (human glioblastoma), as well as a healthy fibroblast cell line (WS-1). Cell viability was assessed using ATP-based luminescence over across a range of concentrations (6.25-200 mu M), revealing dose-dependent cytotoxicity for both the reference drugs (cisplatin, carboplatin, and oxaliplatin) and the newly synthesized complexes (K1-K4 and O1-O4). Among the novel compounds, S-configurated K1 and O1 displayed moderate activity compared to conventional platinum agents. Furthermore, intracellular reactive oxygen species (ROS) generation was measured via H2DCF-DA fluorescence, indicating a concentration-dependent increase in ROS levels for several complexes, particularly K1 and O1, across cancer cell lines. These findings suggest that chiral benzimidazole-based platinum(II) complexes have the potential to serve as scaffolds for developing new metalbased anticancer agents with improved selectivity and mechanistic profiles.