New N'-Arylidene-2-[(4-Nitrophenyl) Piperazin-1-yl]Acetohydrazide Derivatives: Synthesis and Anticancer Activity Investigation

作者：Yurttas Leyla^*; Kaplancikli Zafer A; Gorgulu Kahyaoglu Sennur

来源：Letters in Drug Design and Discovery, 2017, 14(8): 910-917.

DOI：10.2174/1570180814666161207163450

• Antiproliferative
• apoptosis
• cytotoxicity
• hydrazone
• piperazine
• biological activities

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 %.

• 出版日期2017