Background: Compounds bearing ortho-hydroxy N-acyl hydrazone moiety have been
reported with high anticancer activity acting by increasing the enzymatic activity of procaspase-3 in
cancer cells and therefore inducing apoptosis in some tumour models.
Methods: Considering this subunit’s proclivity for anticancer activity we have synthesized novel
N’-arylidene-2-[(4-nitrophenyl)piperazin-1-yl]acetohydrazide derivatives (3a-3n) including N-acyl
hydrazone moiety with a well-known three step synthetic procedure. The antiproliferative activity
of the compounds were investigated using MTT method and xCELLigence real time cell analysis
system against NIH/3T3 (Mouse embryo fibroblast cell line) as healthy cell line and A549 (Human
lung adenocarcinoma ephitelial cell line) as tumour cell line.
Results and Conclusion: The IC50 values of final compounds were determined for 24h and 48h
incubation periods. As a second stage, flow cytometric analysis was performed for selected highly
active compounds (3g, 3i, 3j, 3n) on A549 cell line. Compound 3i bearing 3-chlorophenyl moiety
was detected to cause apoptosis in a ratio of 54.7 %.