Antiproliferative, Cytotoxic, and Apoptotic Effects of New Benzimidazole Derivatives Bearing Hydrazone Moiety

Abstract

in Wiley Online Library (wileyonlinelibrary.com).In order to take the advantages of the anticancer properties of benzimidazoles and hydrazones, we synthesized new 4-(5-chloro-1H-benzimidazol-2-yl)-benzoic acid benzylidene hydrazide derivatives (3a-3t) and evaluated their anticancer activity against A549 (human lung adenocarcinoma) and MCF-7 (human breast adenocarcinoma) cells. The structures of the compounds (3a-3t) were confirmed by IR, 1 H-NMR, 13 C-NMR, mass spectroscopy, and elemental analyses. Antiproliferative activities of the compounds were evaluated using MTT assay, BrdU method, and flow cytometric analysis. In addition, with purpose of determining selectivity the cytotoxic activities of the final compounds were screened against healthy NIH3T3 cell line (mouse vembryonic fibroblast cells). Among the tested compounds 3e and 3f showed significant cytotoxic activity against A549 and MCF-7 cancer cells with an IC 50 value of 0.0316 μM. Furthermore, compound 3p showed remarkable cytotoxic activity against MCF-7 comparing with standard drug cisplatin. Annexin V-FITC assay also suggested that this compounds induced cell death by apoptosis.

Synthesis, anticancer evaluation and molecular docking studies of new benzimidazole- 1,3,4-oxadiazole derivatives as human topoisomerase types I poison

“…OD of the wells were determined at 492 nm. Proliferation of control cells was assessed as 100% and growth inhibition % of cells, treated with test compounds and cisplatin were calculated 34 .…”

A Review on Benzimidazole Heterocyclic Compounds: Synthesis and Their Medicinal Activity Applications

“…Ulviye Acar Cevik et al [68] were tested the anticancer activity of the prepared benzimidazole derivatives. The results showed that the toxic activity of the diseased cells was shown by compounds (4a) and (4b).…”

A Review of Approaches to the Metallic and Non-Metallic Synthesis of Benzimidazole (BnZ) and Their Derivatives for Biological Efficacy

“…Compounds 5a and 5b, when applied to human-lung-cell-line adenocarcinoma, have an IC 50 of 0.0316 μM. Compared with the classical anticancer medicine cisplatin (IC 50 0.045 and 0.052 μM), 5c (4-(6-chloro-1H-benzo[d]imidazol-2-yl)-N′-(2-methoxybenzylidene)benzohydrazide) showed significant cytotoxicity, with an IC 50 of around 0.06 μM [ 84 ]. Elancheran et al synthesized and examined a number of oxo-bBnZ derivatives for their ability to inhibit androgen receptor functions.…”