Twenty-four new dibenzo[b,d]furan–1H-1,2,4-triazole derivatives were synthesized
and investigated for in vitro cytotoxic activity against five tumor cell lines. The results show
that the substitution at 4-position of the 1,2,4-triazole with a benzyl, 4-bromophenacyl or
naphthylacyl group could be crucial for prommoting cytotoxic activity. Especially, compound
28 was found to be the most powerful derivative with IC50 values lower than 3.50 μM against
five investigated tumor cell lines, while compound 19 showed selective activity against
leukemia (HL-60) and breast carcinoma (MCF-7) cell lines with IC50 values of 0.80 and 1.76 μM, respectively. Compound 19 can induce
cell cycle arrest at G2/M phase and apoptosis in SMMC-7721 cells.
Keywords: Dibenzo[b, d]furan, 1, 2, 4-triazolium salts, structure-activity relationships, cell apoptosis.
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