Generic placeholder image

Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

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

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

Volume 14, Issue 8, 2017

Page: [910 - 917] Pages: 8

DOI: 10.2174/1570180814666161207163450

Price: $65


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.

Graphical Abstract

Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy