Design, synthesis, and cytotoxicity of 5-fluoro-2-methyl-6-(4-aryl-piperazin-1-yl) benzoxazoles

Thuraya Al-Harthy, Wajdi Michel Zoghaib, Maren Pflüger, Miriam Schöpel, Kamil Önder, Maria Reitsammer, Harald Hundsberger, Raphael Stoll, Raid Abdel-Jalil*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

11 Citations (Scopus)


To design new compounds suitable as starting points for anticancer drug development, we have synthesized a novel series of benzoxazoles with pharmaceutically advantageous piperazine and fluorine moieties attached to them. The newly synthesized benzoxazoles and their corresponding precursors were evaluated for cytotoxicity on human A-549 lung carcinoma cells and non-cancer HepaRG hepatocyes. Some of these new benzoxazoles show potential anticancer activity, while two of the intermediates show lung cancer selective properties at low concentrations where healthy cells are unaffected, indicating a selectivity window for anticancer compounds.

Original languageEnglish
Article number1290
Issue number10
Publication statusPublished - Oct 1 2016


  • A-549 lung carcinoma cells
  • Benzoxazole
  • Fluorine Cytotoxicity
  • HepaRG hepatocytes
  • Piperazine

ASJC Scopus subject areas

  • Drug Discovery
  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Physical and Theoretical Chemistry
  • Pharmaceutical Science
  • Organic Chemistry


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