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      Cytotoxic activities of some benzothiazole-piperazine derivatives

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      Author
      Gurdal, E.E.
      Durmaz I.
      Cetin-Atalay, R.
      Yarim, M.
      Date
      2015
      Source 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
      Article
      Item Usage Stats
      136
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      169
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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
      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
      Permalink
      http://hdl.handle.net/11693/21381
      Published Version (Please cite this version)
      http://dx.doi.org/10.3109/14756366.2014.959513
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