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
Affiliations
Thuraya Al-Harthy
Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman
Wajdi Michel Zoghaib
Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman
Maren Pflüger
IMC Fachhochschule Krems University of Applied Sciences Krems, Piaristengasse 1, Krems A-3500, Austria
Miriam Schöpel
Biomolecular NMR, Ruhr University of Bochum, Bochum 44780, Germany
Kamil Önder
Research Program for Rational Drug Design in Dermatology and Rheumatolog, Department of Dermatology, General Hospital of Salzburg, Paracelsus Medical, University of Salzburg, Müllner Hauptstraße 48, Salzburg A-5020, Austria
Maria Reitsammer
Research Program for Rational Drug Design in Dermatology and Rheumatolog, Department of Dermatology, General Hospital of Salzburg, Paracelsus Medical, University of Salzburg, Müllner Hauptstraße 48, Salzburg A-5020, Austria
Harald Hundsberger
IMC Fachhochschule Krems University of Applied Sciences Krems, Piaristengasse 1, Krems A-3500, Austria
Raphael Stoll
Biomolecular NMR, Ruhr University of Bochum, Bochum 44780, Germany
Raid Abdel-Jalil
Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman
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.
