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Molecules 2016, 21(10), 1290;

Design, Synthesis, and Cytotoxicity of 5-Fluoro-2-methyl-6-(4-aryl-piperazin-1-yl) Benzoxazoles

Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman
IMC Fachhochschule Krems University of Applied Sciences Krems, Piaristengasse 1, Krems A-3500, Austria
Biomolecular NMR, Ruhr University of Bochum, Bochum 44780, Germany
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
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 5 August 2016 / Revised: 21 September 2016 / Accepted: 22 September 2016 / Published: 27 September 2016
(This article belongs to the Section Medicinal Chemistry)
Full-Text   |   PDF [652 KB, uploaded 27 September 2016]   |  


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. View Full-Text
Keywords: benzoxazole; piperazine; fluorine Cytotoxicity; A-549 lung carcinoma cells; HepaRG hepatocytes benzoxazole; piperazine; fluorine Cytotoxicity; A-549 lung carcinoma cells; HepaRG hepatocytes

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Al-Harthy, T.; Zoghaib, W.M.; Pflüger, M.; Schöpel, M.; Önder, K.; Reitsammer, M.; Hundsberger, H.; Stoll, R.; Abdel-Jalil, R. Design, Synthesis, and Cytotoxicity of 5-Fluoro-2-methyl-6-(4-aryl-piperazin-1-yl) Benzoxazoles. Molecules 2016, 21, 1290.

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