Synthesis, characterization and cytotoxic activity of organoruthenium(II)-halido complexes with 5- chloro-1H-benzimidazole-2-carboxylic acid

Main Authors: Pantić Darko N, Mihajlović-Lalić Ljiljana E., Aranđelović Sandra, Radulović Siniša, Grgurić-Šipka Sanja
Format: Article Journal
Bahasa: eng
Terbitan: , 2019
Subjects:
Online Access: https://zenodo.org/record/4480384
Daftar Isi:
  • Three new ruthenium(II)-arene halido complexes, [(η6-p-cymene) RuX(L)] (1–3), were synthesized in a reaction of [(η6-p-cymene)RuX2]2 with 5-chloro-1H-benzimidazole-2-carboxylic acid (HL) in ethanol (X– = Cl– (1), Br– (2), I– (3)). The complexes were characterized by elemental analysis, mass spectrometry, IR, 1H and 13C NMR spectroscopy. The cytotoxic activity of the ligand precursor and its ruthenium complexes was tested by MTT assay in human cancer cell lines: lung adenocarcinoma (A549), myelogenous leukemia (K562) as well as in one normal human fetal lung fibroblast cell line (MRC-5). The results show that ruthenium(II)-arene complexes possess enhanced cytotoxicity when compared to HL in the range of concentrations up to 300 μM. In terms of halido ligand substitution, cytotoxic activity toward A549 and K562 cell lines in 1–3 serie significantly increased (e.g., IC50 values for K562: 1: 205.76 μM; 2: 174.77 μM; 3: 83.97 μM). All studied compounds were found to be ineffective toward MRC-5. Hydrolysis of 1–3 was followed by UV-vis spectroscopy at 25 °C, revealing ligand-substitution reactions at the Ru(II) center. Compounds 2 and 3 underwent rapid hydrolysis ranging from a few minutes for the aquation to ca. 20 min, confirming typical Ru-arene behavior in aqueous solutions.
  • Granted also by FP7 RegPot project FCUB ERA GA [grant number 256716] Supplementary material: https://www.tandfonline.com/doi/suppl/10.1080/00958972.2019.1583332