In this study we report the synthesis and preliminary evaluation of a series of six 2-aryl-5(6)-nitro-1H-benzimidazole derivatives (1-6) as potential anticancer agents. Cytotoxicity was evaluated against seven human neoplastic cell lines using the MTT assay. Compound 6 [2-(4-chloro-3-nitrophenyl)-5(6)-nitro-1H-benzimidazole] was the most active of the series, showing an IC_50 of 28 nM against the A549 cell line. This compound displayed a selective in vitro cytotoxic activity index (>700) in non neoplastic HACAT cells (IC_50 = 22.2 μM). Compounds 3 and 6 induce arrest in the S phase of the cell cycle, and compounds 1-6 induce apoptosis in the K562 cell line. Compound 6 induces poly (ADP-ribose) polymerase (PARP) inhibition activity as a potential mechanism of action. These results suggest that compound 6 could be a potent anticancer agent. Compound 3 displayed the best inhibitory activity against PARP with an IC_50 value of 0.05 μM, compared to the activity shown by the positive control 3-aminobenzamide (IC_50 = 28.5 μM).
Dong Hun Lee ,Sung Hyun Kim ,Kyong Hoon Ahn ,Seok Kyun Kim ,Jong Min Choi ,Jung Eun Ji ,Jong Hoon Won ,Yang Hui Park ,Chaemin Lim ,Sanghee Kim ,Dae Kyong Kim
대표어
한국학술지인용색인(NRF)
