Design, Synthesis, and Cytotoxicity of 5-Fluoro-2-methyl-6-(4-aryl-piperazin-1-yl) Benzoxazoles.
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.
Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman. thurayalharthi@gmail.com.
Thuraya
T
Al-Harthy
Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman. zoghaibw@squ.edu.om.
Wajdi Michel
WM
Zoghaib
IMC Fachhochschule Krems University of Applied Sciences Krems, Piaristengasse 1, Krems A-3500, Austria. maren.pflueger@fh-krems.ac.at.
Maren
M
Pflüger
Biomolecular NMR, Ruhr University of Bochum, Bochum 44780, Germany. miriam.schoepel@ruhr-uni-bochum.de.
Miriam
M
Schöpel
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. oender@procomcure.com.
Kamil
K
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. m.reitsammer@salk.at.
Maria
M
Reitsammer
IMC Fachhochschule Krems University of Applied Sciences Krems, Piaristengasse 1, Krems A-3500, Austria. harald.hundsberger@fh-krems.ac.at.
Harald
H
Hundsberger
Biomolecular NMR, Ruhr University of Bochum, Bochum 44780, Germany. raphael.stoll@ruhr-uni-bochum.de.
Raphael
R
Stoll
Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman. jalil@squ.edu.om.
Raid
R
Abdel-Jalil
A-549 lung carcinoma cells; HepaRG hepatocytes; benzoxazole; fluorine Cytotoxicity; piperazine
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