Design, synthesis, biological evaluation, and in silico studies of novel N-substituted-2-(3,4,5-trimethoxyphenyl)-1H-benzo[d]imidazole-6-carboxamides as promising anticancer agents.

ABSTRACT: Novel benzimidazole-based derivatives were synthesized and their cytotoxic activities were evaluated against two human cancer cells, SW480 and A549, and the normal human MRC-5 cells, using the MTT assay. N-(2,4-Dimethoxyphenyl)-2-(3,4,5-trimethoxyphenyl)-1H-benzo[d]imidazole-6-carboxamide (5o) showed excellent cytotoxicity with IC₅₀ values of 0.15 ± 0.01 and 3.68 ± 0.59 μM against A549 and SW480. Compound 5o had 38.5-, 62.9- and 3.1-fold superior cytotoxicity than cisplatin (IC₅₀ = 5.77 ± 1.60 μM), etoposide (IC₅₀ = 9.44 ± 1.98 μM), and doxorubicin (IC₅₀ = 0.46 ± 0.02 μM), respectively against A549 cells. Moreover, 5o exhibited high selectivity towards A549 (SI = 794.6) and SW480 (SI = 32.4) cancer cells compared with the nor

SUBMITTER: Dastyafteh N 

PROVIDER: S-EPMC11536976 | biostudies-literature | 2024 Nov

REPOSITORIES: biostudies-literature