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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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

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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

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

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

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Department of Molecular Biology and Genetics