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.
Letters in Drug Design & Discovery
Title:New N’-Arylidene-2-[(4-Nitrophenyl)Piperazın-1-yl]Acetohydrazide Derivatives: Synthesis and Anticancer Activity Investigation
Volume: 14 Issue: 8
Author(s): Leyla Yurttas*, Zafer A. Kaplancikli and Sennur Gorgulu-Kahyaoglu
Affiliation:
- Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Eskisehir,Turkey
Keywords: Antiproliferative, apoptosis, cytotoxicity, hydrazone, piperazine, biological activities.
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 %.Export Options
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Cite this article as:
Yurttas Leyla*, Kaplancikli A. Zafer and Gorgulu-Kahyaoglu Sennur, New N’-Arylidene-2-[(4-Nitrophenyl)Piperazın-1-yl]Acetohydrazide Derivatives: Synthesis and Anticancer Activity Investigation, Letters in Drug Design & Discovery 2017; 14 (8) . https://dx.doi.org/10.2174/1570180814666161207163450
DOI https://dx.doi.org/10.2174/1570180814666161207163450 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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