Cytotoxic activities of some benzothiazole-piperazine derivatives

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

Journal of Enzyme Inhibition and Medicinal Chemistry, vol.30, no.4, pp.649-654, 2015 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 30 Issue: 4
  • Publication Date: 2015
  • Doi Number: 10.3109/14756366.2014.959513
  • Journal Name: Journal of Enzyme Inhibition and Medicinal Chemistry
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.649-654
  • Keywords: Anticancer, benzothiazole, cytotoxicity, piperazine, sulphorodamine B
  • Istanbul Medipol University Affiliated: No


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.