Cytotoxic activities of some benzothiazole-piperazine derivatives

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Cytotoxic activities of some benzothiazole-piperazine derivatives.pdf (869.97 KB)

Date

2015

Authors

Gurdal, E.E.
Durmaz I.
Cetin-Atalay, R.
Yarim, M.

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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.

Source Title

Journal of Enzyme Inhibition and Medicinal Chemistry

Publisher

Taylor and Francis Ltd

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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

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http://hdl.handle.net/11693/21381

Published Version (Please cite this version)

http://dx.doi.org/10.3109/14756366.2014.959513

Collections

Scholarly Publications - Molecular Biology and Genetics

Language

English

Type

Article