Antitumor Activity In Vitro Provided by N-Alkyl-Nitroimidazole Compounds

Cancer is one of the most common diseases in the world, with over 18 million new cases estimated in 2018. Many of the drugs used for cancer can have significant adverse effects and variable effectiveness. Nitroimidazoles are prodrugs that usually have shown antimicrobial activity specifically antiparasitic. However, its antitumor activity in vitro has barely been explored.

The aim of this study is to determine the influence of the length of the substituted N-alkyl chain in the imidazole ring on the antitumor activity in vitro.

Four nitroimidazoles were obtained by chemical synthesis varying the length of the substituted N-alkyl chain from methyl to butyl. The antitumor activity of N-alkyl-nitroimidazoles was evaluated by MTT assay employing two tumor cell lines (MDA-MB231 and A549).

In this study, it was reported that N-alkyl nitroimidazoles exhibited an LC₅₀ as low as 16.7 µM in breast tumor cells MDA-MB231 while in normal Vero kidney cells, the LC₅₀ was around 30 µM. It was also reported that the length of the substituted N-Alkyl chain in the imidazole ring affects the antitumoral activity in A549 lung cells.

Increasing the length of the substituted N-Alkyl chain in the imidazole ring decreased the antitumor activity against only A549 cancer cells. N-alkyl nitroimidazoles exhibited considerable selectivity towards tumor cell lines.