In vitro Selective Effect of Imidazole Derivatives as Inhibitors of Human Laryngeal Carcinoma

Vasyl Kovalishyn (Laboratory of Biomedical Research, V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine, Kyiv-02094 (Ukraine))
Sergiy Rogalsky (Laboratory of Modification of Polymers, V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine, Kyiv-02160 (Ukraine))
Diana Hodyna (Laboratory of Biomedical Research, V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine, Kyiv-02094 (Ukraine))
Petro Borysko (Laboratory of Biomedical Research, V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine, Kyiv-02094 (Ukraine) Bienta/Enamine Ltd., Kyiv-02094 (Ukraine))
Larysa Metelytsia (Laboratory of Biomedical Research, V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine, Kyiv-02094 (Ukraine))

Bioactivities
Vol. 3 No. 2 (2025): Bioactivities

Laryngeal cancer represents a significant portion of head and neck malignancies, greatly affecting quality of life. Despite advancements in treatment, late-stage mortality remains high. The HEp-2 cell line, derived from human laryngeal carcinoma, serves as an in vitro model for studying this cancer. We present in vitro results highlighting the activity of imidazole-based ionic liquids and lysosomotropic detergents as selective inhibitors of laryngeal cancer growth using the HEp-2 cell line, alongside non-oncogenic MRC-5 and HEK-293 cell lines. A comparative analysis of the selectivity coefficients reflecting the action of these imidazole derivatives on HEp-2 cancer cells, compared to their effects on MRC-5 fibroblasts and HEK-293 kidney cells, revealed that the compounds 1-dodecyl-3-methylimidazolium chloride, 1-decyloxycarbonylmethylimidazole, and 1-dodecyloxycarbonylmethyl-3-methylimidazolium chloride appear to be promising candidates with selective activity against laryngeal cancer, with anticancer selectivity coefficients ranging from 2.8 to 11.5 and 2.2 to 20.1, respectively. Especially promising is 1-dodecylimidazole, which has an average selectivity coefficient of 47,675 based on IC₅₀ values for the two non-oncogenic cell lines. Notably, the selectivity coefficients of these compounds were significantly higher—by two or more times—than those of the drug cisplatin.