Design, synthesis and anticancer activity of 5-((2-(4-bromo/chloro benzoyl) benzofuran-5-yl) methyl)-2-((1-(substituted)-1H-1,2,3-triazol-4-yl)methoxy)benzaldehyde analogues

Abstract

Novel 5-((2-(4-bromo/chloro benzoyl) benzofuran-5-yl) methyl)-2-((1-(substituted)-1H-1,2,3-triazol-4-yl)methoxy)benzaldehyde analogues about twenty-one were synthesized all through standard chemical procedures. The structure of the compounds were confirmed by ¹H NMR, ¹³C NMR and Mass spectral analysis after purification. All the compounds were screened for In Vitro lung and cervical cancer activity against A-549 and HeLa cell lines, respectively, by MTT assay protocol using various nanomolar (nM) concentrations. IC₅₀ value were calculated from cell viability data. 2-(trifluoromethyl)benzyl substituted derivative presented outstanding activity against both the cell lines compared to standard drug doxorubicin. The methoxy, chloro, fluoro and formyl substituted analogues showed a moderate activity and whereas methyl substituted analogues activity was poor. The morphological deformation of both cell lines by best IC₅₀ value analogues proved as potent inhibitors of cancer cells growth. Molecular docking studies were performed against extracellular signal-regulated kinase 2 and fibroblast growth factor receptor 2 these results are incredibly in agreement with the investigational data.

Keywords: 1,2,3-Triazole; Benzofuran; Cervical cancer; Lung cancer; Molecular docking; PyRx.