Cytotoxic activities of some benzothiazole-piperazine derivatives

Date
2015
Authors
Gurdal, E.E.
Durmaz I.
Cetin-Atalay, R.
Yarim, M.
Advisor
Supervisor
Co-Advisor
Co-Supervisor
Instructor
Source Title
Journal of Enzyme Inhibition and Medicinal Chemistry
Print ISSN
14756366
Electronic ISSN
Publisher
Taylor and Francis Ltd
Volume
30
Issue
4
Pages
649 - 654
Language
English
Type
Article
Journal Title
Journal ISSN
Volume Title
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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 GI50 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 subG1 phase. © 2014 Informa UK Ltd. All rights reserved.

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Keywords
Anticancer, benzothiazole, 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
Citation
Published Version (Please cite this version)