Abstract
Cancer is one of the leading causes of death in the world. In this study, a series of novel aryl-naphthalene lignans were synthesized and the inhibitory effects of all compounds on cancer cells growth were investigated. The target compounds were structurally characterized by 1H NMR, 13C NMR, IR and HRMS. The IC50 of these compounds on three tumor cell lines A549, SW480, KB and one normal cell line HEK293 were obtained by MTT assay. Compound 6′i, which has a para-methyl on the D-ring indicated potent anti-tumor activities and the IC50 of this compound on KB cells was 18.9 μM. But this compound showed low cytotoxicity on normal cell line HEK293. Furthermore, fluorescent double staining indicated that compound 6′i induced apoptosis of KB cells. Western blot analysis showed Compound 6′i increased the expression of cleaved-caspase-3 and bax, reduced the expression of bcl-2.
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