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Cytotoxic activities of some benzothiazole-piperazine derivatives

Enise Ece Gurdal1, Irem Durmaz, Rengul Cetin-Atalay

  • 1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University , Kayisdagi, Istanbul , Turkey and.

Journal of Enzyme Inhibition and Medicinal Chemistry
|October 22, 2014
PubMed

Insights

Ten novel benzothiazole-piperazine derivatives were synthesized and evaluated for anticancer properties. Compound 1d demonstrated significant cytotoxicity against liver, breast, and colon cancer cells, inducing apoptosis via cell cycle arrest.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Cancer Biology

Background:

  • Benzothiazole and piperazine scaffolds are recognized for their diverse pharmacological activities.
  • Developing novel anticancer agents is crucial for improving patient outcomes in oncology.

Purpose of the Study:

  • To synthesize and characterize new benzothiazole-piperazine derivatives.
  • To evaluate the in vitro cytotoxic activities of these compounds against various human cancer cell lines.
  • To investigate the mechanism of action of the most potent derivative.

Main Methods:

  • Synthesis and characterization of ten benzothiazole-piperazine derivatives.
  • In vitro cytotoxicity screening using the sulphorhodamine B assay against hepatocellular (HUH-7), breast (MCF-7), and colorectal (HCT-116) cancer cell lines.
  • Apoptosis analysis of the lead compound using Hoechst Staining and Fluorescence-Activated Cell Sorting (FACS).

Main Results:

  • Most synthesized benzothiazole-piperazine derivatives exhibited cytotoxic activity against the tested cancer cell lines.
  • Compound 1d displayed high cytotoxicity across all evaluated cancer cell lines (HUH-7, MCF-7, HCT-116).
  • Compound 1d was found to induce apoptosis through cell cycle arrest at the subG1 phase.

Conclusions:

  • The synthesized benzothiazole-piperazine derivatives hold potential as anticancer agents.
  • Compound 1d is a promising lead compound for further development in cancer therapy.
  • The mechanism of action for compound 1d involves the induction of apoptosis via cell cycle arrest.
Keywords:
Anticancerbenzothiazolecytotoxicitypiperazinesulphorodamine B

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