Synthesis and In Vitro Anticancer Evaluation of Some Benzimidazolium Salts

Abstract

A series of benzimidazolium salts having 2‐cyanobenzyl (2–6), 2‐(4‐nitrophenyl)ethyl (7–10), (1,3‐dioxoisoindolin‐2‐yl)butyl (11–17) or N‐methylphthalimide (18–22) substitution were synthesized and characterized by spectroscopic and analytical techniques. The in vitro cytotoxic activity of these salts was tested against human colon cancer (DLD‐1), human breast cancer (MDA‐MB‐231), and normal human noncancerous embryonic kidney (HEK‐293T) cell lines using the MTT assay method. The viability rates of the cells were determined by confocal microscopy. The majority of the newly synthesized compounds, with the exception of compounds 2, 3, 8, 11, 12, and 17, displayed high cytotoxic activity against cancerous cells. In fact, compounds 6 and 7 exhibited better results than the positive control drugs, cisplatin and busulfan, against the MDA‐MB‐231 cells. Therefore, compounds 6 and 7 could be considered as anticancer drug candidates for further development.

Synthesis, Characterization, and Antiproliferative Activity Studies of Novel Benzimidazole‐Imidazopyridine Hybrids as DNA Groove Binders

“…Compounds ( 1 and 2 ) were tested as anticancer agents against HepG2, MDA‐MB‐231 and DLD‐1 cell lines using the MTT assay method for 48 h . Under the same experimental conditions, cisplatin was used as a positive control drug.…”

Design, synthesis, characterization, and in vitro cytotoxic activity evaluation of 1,2‐disubstituted benzimidazole compounds

“…The cytotoxic activity studies were conducted according to literature procedures. [20,21] MCF-7 and HepG2 cells were cultured in DMEM including high glucose supplemented with 1% penicillin streptomycin and 10% FBS. The cell seeding was done in a density of 4 × 10 3 cells/well into sterile 96-well plates and maintained at 37 C for 24 h. MCF-7 and HepG2 cells were exposed to synthesized compounds (2-4) at nine different concentrations (200-0.5 μM) and six dissimilar concentrations ranging from 200 to 5 μM, respectively.…”

Synthesis, characterization, duplex‐DNA interactions, and anticancer activities of novel octahedral [Ni(phen)2(dppz‐idzo)]2+ and [Co(phen)2(dppz‐idzo)]3+ complexes

“…The cytotoxic activity procedures reported previously were applied in this study. [31][32][33][34][35] The HepG2, MDA-MB-231, MCF-7, and DLD-1 cell lines were cultured in DMEM supplemented with 10% FBS, 1% GlutaMAX, and 1% penicillin-streptomycin. The cells were seeded onto sterile 96-well plates at a density of 5 × 10 3 cells per well.…”