Synthesis of new 5-chloro-6-methoxy-2-[4-(substituted)benzylidene]-2,3-dihydro-1H-inden-1-one derivatives and investigation of their biological effects

Due to the increased number of cancer patients, the development of new and potent anticancer agents with low toxicity has gained great importance. Chalcones are natural or synthetic flavonoid compounds. Recent studies indicate that chalcone compounds have fairly high anticancer activity. In this study, new chalcone derivatives were obtained via the reaction of 5-chloro-6-methoxy-2,3-dihydro-1H-inden-1-one with p-substituted benzaldehyde derivatives. The cytotoxic effects of the synthesized compounds on MCF-7 human breast adenocarcinoma and HeLa human cervix carcinoma cell lines were evaluated using MTT assay. In addition, the toxicities of the compounds against NIH/3T3 mouse embryonic fibroblast cell line were investigated. The effective anticancer compounds were evaluated for their DNA synthesis inhibition effects on both cell lines. Compound 10 caused more DNA synthesis inhibition on MCF-7 cells, whereas compound 3 caused more DNA synthesis inhibition on HeLa cells. The apoptotic effects of the most effective compounds on both cell lines were investigated. Compounds 2 and 3 were determined as the most apoptotic compounds against HeLa cells, whilst compounds 7 and 10 showed apoptotic activity against MCF-7 cells. Besides, compound 2 was found as the compound that caused the most caspase-3 activation on HeLa cells.