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      Synthesis and anticancer activity evaluation of some benzothiazole-piperazine derivatives

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      Author(s)
      Gurdal, E.E.
      Buclulgan, E.
      Durmaz I.
      Cetin-Atalay, R.
      Yarim, M.
      Date
      2015
      Source Title
      Anti-Cancer Agents in Medicinal Chemistry
      Print ISSN
      18715206
      Publisher
      Bentham Science Publishers B.V.
      Volume
      15
      Issue
      3
      Pages
      382 - 389
      Language
      English
      Type
      Article
      Item Usage Stats
      163
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      181
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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. Aroyl substituted compounds 1h and 1j were found to be the most active derivatives. In addition, further investigation of compounds 1h and 1j by Hoechst staining and FACS revealed that these compounds cause apoptosis by cell cycle arrest at subG1 phase. © 2015 Bentham Science Publishers.
      Keywords
      Anticancer
      Apoptosis
      Benzothiazole
      Cytotoxicity
      Piperazine
      Sulphorhodamine B
      benzothiazole derivative
      flurouracil
      n (4 methyl 1,3 benzothiazol 2 yl) 2 (4 acetylpiperazin 1 yl)acetamide
      n (4 methyl 1,3 benzothiazol 2 yl) 2 (4 benzoylpiperazin 1 yl)acetamide
      n (4 methyl 1,3 benzothiazol 2 yl) 2 [4 (2 furoyl)piperazin 1 yl]acetamide
      n (4 methylbenzothiazol 2 yl) 2 (4 chlorobenzylpiperazin 1 yl)acetamide
      n (4 methylbenzothiazol 2 yl) 2 (4 methylpiperazin 1 yl)acetamide
      n (4 methylbenzothiazol 2 yl) 2 [1 (4 methylphenyl)piperazine 1 yl)acetamide
      n (4 methylbenzothiazol 2 yl) 2 [4 (2 hydroxyphenyl)piperazin 1 yl)]acetamide
      n (4 methylbenzothiazol 2 yl) 2 [4 (3,4 dichlorophenyl)piperazin 1 yl]acetamide
      n (4 methylbenzothiazol 2 yl) 2 [4 (4 fluorophenyl)piperazin 1 yl]acetamide
      n (4 methylbenzothiazol 2 yl) 2 [4 (4 nitrophenyl)piperazin 1 yl]acetamide
      piperazine derivative
      unclassified drug
      antineoplastic agent
      benzothiazole
      benzothiazole derivative
      piperazine
      piperazine derivative
      antineoplastic activity
      apoptosis
      Article
      bioassay
      carbon nuclear magnetic resonance
      cell cycle arrest
      controlled study
      cytotoxicity
      drug structure
      drug synthesis
      fluorescence activated cell sorting
      Hoechst staining
      human
      human cell
      infrared spectroscopy
      proton nuclear magnetic resonance
      sulphorhodamine B assay
      cell cycle
      cell death
      cell proliferation
      chemical structure
      chemistry
      dose response
      drug effects
      drug screening
      HCT116 cell line
      MCF 7 cell line
      structure activity relation
      synthesis
      tumor cell culture
      Antineoplastic Agents
      Benzothiazoles
      Cell Cycle
      Cell Death
      Cell Proliferation
      Dose-Response Relationship, Drug
      Drug Screening Assays, Antitumor
      HCT116 Cells
      Humans
      MCF-7 Cells
      Molecular Structure
      Piperazines
      Structure-Activity Relationship
      Tumor Cells, Cultured
      Permalink
      http://hdl.handle.net/11693/24159
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