2-Phenyl substituted Benzimidazole derivatives: Design, synthesis, and evaluation of their antiproliferative and antimicrobial activities

نویسندگان

چکیده

The inability to meet the desired outcomes of anticancer treatment and decrease in success bacterial fungal infections accelerated research these areas. Our group has conducted numerous studies, especially on benzimidazole ring systems’ antiproliferative antimicrobial activities. In this study, activity compounds was tested against A549, A498, HeLa, A375, HepG2 cancer cell lines by MTT assay. All exhibited good potent all lines. Compounds 6-chloro-2-(4-fluorobenzyl)-1H-benzo[d]imidazole (30) 6-chloro-2-phenethyl-1H-benzo[d]imidazole (46) were active HeLa A375 with IC50 values range 0.02–0.04 µM. contrast, 6-chloro-2-((p-tolyloxy)methyl)-1H-benzo[d]imidazole (67) 5(6)-chloro-2-((4-hydroxyphenoxy)methyl)-1H-benzimidazole (68) A549 A498 an value 0.08 These (30, 46, 67, 68) less toxic normal human cells than positive control compound methotrexate, which screened determine its toxicity (HEK293). second part demonstrate their properties. moderate bacteria fungi. However, some phenoxy methyl derivatives 5-chloro-2-((4-chlorophenoxy)methyl)-1H-benzo[d]imidazole (69) 5,6-dichloro-2-((4-chlorophenoxy)methyl)-1H-benzo[d]imidazole (74) most Candida (<3.90 µg/mL). Molecular docking studies carried out certain proteins order identify potential targets effects synthesized compounds. scores found be significantly compatible results.

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ژورنال

عنوان ژورنال: Medicinal Chemistry Research

سال: 2022

ISSN: ['1554-8120', '1054-2523']

DOI: https://doi.org/10.1007/s00044-022-02900-3