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

T. Al-Harthy; W.M. Zoghaib; M. Pflüger; M. Schöpel; K. Önder; M. Reitsammer; H. Hundsberger; R. Stoll; R. Abdel-Jalil

doi:10.3390/molecules21101290

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

T. Al-Harthy, W.M. Zoghaib, M. Pflüger, M. Schöpel, K. Önder, M. Reitsammer, H. Hundsberger, R. Stoll, R. Abdel-Jalil

Institute Biotechnology

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Article number	1290
Journal	Molecules
Volume	21
Issue number	10
DOIs	https://doi.org/10.3390/molecules21101290
Publication status	Published - 27 Sept 2016

Keywords

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

IMC Research Focuses

Medical biotechnology

ÖFOS 2012 - Austrian Fields of Study

304005 Medical biotechnology

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.3390/molecules21101290

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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.",

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T1 - Design, synthesis, and cytotoxicity of 5-fluoro-2-methyl-6-(4-aryl-piperazin-1-yl) benzoxazoles

AU - Al-Harthy, T.

AU - Zoghaib, W.M.

AU - Pflüger, M.

AU - Schöpel, M.

AU - Önder, K.

AU - Reitsammer, M.

AU - Hundsberger, H.

AU - Stoll, R.

AU - Abdel-Jalil, R.

PY - 2016/9/27

Y1 - 2016/9/27

N2 - 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.

AB - 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.

KW - A-549 lung carcinoma cells

KW - Benzoxazole

KW - Fluorine Cytotoxicity

KW - HepaRG hepatocytes

KW - Piperazine

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U2 - 10.3390/molecules21101290

DO - 10.3390/molecules21101290

M3 - Article

C2 - 27689973

SN - 1420-3049

VL - 21

JO - Molecules

JF - Molecules

IS - 10

M1 - 1290

ER -

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

Abstract

Keywords

IMC Research Focuses

ÖFOS 2012 - Austrian Fields of Study

UN SDGs

Access to Document

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