Cytotoxic activities of some benzothiazole-piperazine derivatives
Author
Gurdal, E.E.
Durmaz I.
Cetin-Atalay, R.
Yarim, M.
Date
2015Source Title
Journal of Enzyme Inhibition and Medicinal Chemistry
Print ISSN
14756366
Publisher
Taylor and Francis Ltd
Volume
30
Issue
4
Pages
649 - 654
Language
English
Type
ArticleItem Usage Stats
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Abstract
Synthesis, characterization and cytotoxic activities of ten benzothiazole-piperazine derivatives were reported. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. Based on the GI<inf>50</inf> values of the compounds, most of the benzothiazole-piperazine derivatives are active against HUH-7, MCF-7 and HCT-116 cancer cell lines. Compound 1d is highly cytotoxic against all tested cancer cell lines. Further investigation of compound 1d by Hoechst Staining and Fluorescence-Activated Cell Sorting Analysis (FACS) revealed that this compound causes apoptosis by cell cycle arrest at subG<inf>1</inf> phase. © 2014 Informa UK Ltd. All rights reserved.
Keywords
Anticancerbenzothiazole
cytotoxicity
piperazine
sulphorodamine B
antineoplastic agent
benzothiazole derivative
fluorouracil
n (6 ethoxybenzothiazol 2 yl) 2 [4 (o chlorophenyl)piperazinyl]acetamide
n (6 ethoxybenzothiazol 2 yl) 2 [4 (o cyanophenyl)piperazinyl]acetamide
n (6 ethoxybenzothiazol 2 yl) 2 [4 (p cyanophenyl)piperazinyl]acetamide
n (6 ethoxybenzothiazol 2 yl) 2 [4 (p toluyl)piperazinyl]acetamide
n (6 methylbenzothiazol 2 yl) 2 (4 cyclohexylpiperazinyl)acetamide
n (6 methylbenzothiazol 2 yl) 2 [4 (2 methoxyethyl)piperazinyl]acetamide
n (6 methylbenzothiazol 2 yl) 2 [4 (2 methoxyphenyl)piperazinyl]acetamide
n (6 methylbenzothiazol 2 yl) 2 [4 (3,4 dichlorophenyl)piperazinyl]acetamide
n (6 methylbenzothiazol 2 yl) 2 [4 (4 chlorobenzyl)piperazinyl]acetamide
n (6 methylbenzothiazol 2 yl) 2 [4 (pyridin 4 yl)piperazinyl]acetamide
piperazine derivative
sulforhodamine B
unclassified drug
apoptosis
Article
cancer cell line
cell cycle arrest
cell cycle G1 phase
chemical structure
controlled study
drug cytotoxicity
drug synthesis
fluorescence activated cell sorting
human
human cell
human cell culture
in vitro study
priority journal
proton nuclear magnetic resonance