Synthesis of newer substituted chalcone linked 1,2,3-triazole analogs and evaluation of their cytotoxic activities

Abstract

An innovative heterocyclic biologically active chalcone 1,2,3-triazole analogs (6a–j) were prepared to extract excellent yields by coupling the substituted aryl azides (5a–5j) and 5-ethynyl-1,2,3-trimethoxybenzene, by using the method of Huisgen azide–alkyne cycloaddition. The typically synthesized analogs were elucidated by IR, 1H-nuclear magnetic resonance (NMR), 13C-NMR, and Electron spray ionization (ESI)-mass spectroscopy and tested for their cytotoxicity effectiveness in MTT assays against the A549 lung cancer cells. The cytotoxic studies suggested that a few analogs showed moderate to good activities. The compounds 6i and 6c showed low cytotoxicity against the A549 cell line among 12 analogs, the values of IC50 were displayed in the range of 65.05 ± 1.12 and 71.56 ± 1.29 µM, respectively. The compound 6j showed slightly less cytotoxicity but showed good selectivity against A549 cell lines.