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Molecules. 2016 Sep 27;21(10). pii: E1290.

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

Author information

1
Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman. thurayalharthi@gmail.com.
2
Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman. zoghaibw@squ.edu.om.
3
IMC Fachhochschule Krems University of Applied Sciences Krems, Piaristengasse 1, Krems A-3500, Austria. maren.pflueger@fh-krems.ac.at.
4
Biomolecular NMR, Ruhr University of Bochum, Bochum 44780, Germany. miriam.schoepel@ruhr-uni-bochum.de.
5
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.
6
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.
7
IMC Fachhochschule Krems University of Applied Sciences Krems, Piaristengasse 1, Krems A-3500, Austria. harald.hundsberger@fh-krems.ac.at.
8
Biomolecular NMR, Ruhr University of Bochum, Bochum 44780, Germany. raphael.stoll@ruhr-uni-bochum.de.
9
Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman. jalil@squ.edu.om.

Abstract

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.

KEYWORDS:

A-549 lung carcinoma cells; HepaRG hepatocytes; benzoxazole; fluorine Cytotoxicity; piperazine

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