Antiproliferative activities of 2-hydroxyethyl substituted benzimidazolium salts and their palladium complexes against human cancerous cell lines

Abstract

Benzimidazolium salts (1a and 1b) and respective palladium complexes (2a and 2b) were prepared and characterized with ¹H and ¹³C NMR, IR, elemental analysis as well as HRMS (for 2a). All target compounds were screened as potential anticancer agents against human cell lines for assessing their cytotoxicity. Heterocyclic organic compounds (1a and 1b) showed more cytotoxic activity than their complexes (2a and 2b) in the tested two cell lines. Particularly, a benzimidazolium salt including a 4-methylbenzyl group had a high cytotoxic potency towards MDA-MB-231 and DLD-1 cell lines with IC₅₀ values comparable to a well-known anticancer drug cisplatin, which is generally used in clinical studies. Furthermore, a compound namely 1-(2-hydroxyethyl)-3-(2,3,4,5,6-pentamethylbenzyl)-1H-benzo[d]imidazol-3-ium bromide was found to be more cytotoxic activity in MDA-MB-231 cell line compared to cisplatin with following IC₅₀ value of 7.59 ± 0.68 μM.

GRAPHICAL ABSTRACT

Keywords:

• Anticancer
• benzimidazolium salts
• cytotoxic activity
• N-heterocyclic carbene
• PEPPSI

Acknowledgments

I would like to express my heartfelt gratitude to Erciyes University, Genom and Stem Cell Center (ERU GENKOK) for giving me study places for cell culture. I would also like to thank Yahuza Nantomah Abdulai for reading the manuscript and correcting its grammatical mistakes.

Disclosure statement

The author declares that no conflict of interest is associated with this work.