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

Author(s): Leyla Yurttas*, Zafer A. Kaplancikli, Sennur Gorgulu-Kahyaoglu.

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 8 , 2017

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Abstract:

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 %.

Keywords: Antiproliferative, apoptosis, cytotoxicity, hydrazone, piperazine, biological activities.

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Article Details

VOLUME: 14
ISSUE: 8
Year: 2017
Page: [910 - 917]
Pages: 8
DOI: 10.2174/1570180814666161207163450
Price: $58

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