A series of N-benzyl-9(10H)-acridinones were synthesized and tested for their antitumor activities in vitro against HepG2 cells.Assay-based antiproliferative activity study using HepG2 cell lines revealed that several compounds had significant effects on cytotoxicity, among which compound 5h was found to be the most active compound with IC50 at about 1.33 μM using the MTT assay. The antitumor effect of compound 5h is believed to be due to the induction of apoptosis, which was further confirmed by Hoechst 33258 fluorescence staining, agarose gel electrophoresis and Annexin VFITC/ PI staining assay using flow cytometry analysis. Above all, compound 5h would be a potential anticancer agent which deserves further research.
Keywords: Acridinone, Antiproliferative activity, Apoptosis, HepG2 cell, N-benzyl-acridinone, antiproliferative, agarose gel electrophoresis, cytotoxicity, Annexin V-FITC/PI staining assay, chemotherapeutic agents, Hepatocellular carcinoma (HCC), metastasis, hydrophobic, Jourdan, –, Ulmann copper-catalysed condensation
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