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Anti-Cancer Activity of Phenyl and Pyrid-2-yl 1,3-Substituted Benzo[1,2,4]triazin-7-ones and Stable Free Radical Precursors
Cell viability studies for benzo[1,2,4]triazin-7-ones and 1,2,4-benzotriazinyl (Blatter-type) radical precursors are described with comparisons made with 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). All of the stable free radicals were several orders of magnitude less cytotoxic than the benzo[1,2,4...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017941/ https://www.ncbi.nlm.nih.gov/pubmed/29510488 http://dx.doi.org/10.3390/molecules23030574 |
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author | Keane, Lee-Ann J. Mirallai, Styliana I. Sweeney, Martin Carty, Michael P. Zissimou, Georgia A. Berezin, Andrey A. Koutentis, Panayiotis A. Aldabbagh, Fawaz |
author_facet | Keane, Lee-Ann J. Mirallai, Styliana I. Sweeney, Martin Carty, Michael P. Zissimou, Georgia A. Berezin, Andrey A. Koutentis, Panayiotis A. Aldabbagh, Fawaz |
author_sort | Keane, Lee-Ann J. |
collection | PubMed |
description | Cell viability studies for benzo[1,2,4]triazin-7-ones and 1,2,4-benzotriazinyl (Blatter-type) radical precursors are described with comparisons made with 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). All of the stable free radicals were several orders of magnitude less cytotoxic than the benzo[1,2,4]triazin-7-ones. The synthesis and evaluation of two new pyrid-2-yl benzo[1,2,4]triazin-7-ones are described, where altering the 1,3-substitution from phenyl to pyrid-2-yl increased cytotoxicity against most cancer cell lines, as indicated using National Cancer Institute (NCI) one-dose testing. COMPARE analysis of five-dose testing data from the NCI showed very strong correlations to the naturally occurring anti-cancer compound pleurotin. COMPARE is program, which analyzes similarities in cytotoxicity data of compounds, and enables quantitative expression as Pearson correlation coefficients. Compounds were also evaluated using the independent MTT assay, which was compared with SRB assay data generated at the NCI. |
format | Online Article Text |
id | pubmed-6017941 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-60179412018-11-13 Anti-Cancer Activity of Phenyl and Pyrid-2-yl 1,3-Substituted Benzo[1,2,4]triazin-7-ones and Stable Free Radical Precursors Keane, Lee-Ann J. Mirallai, Styliana I. Sweeney, Martin Carty, Michael P. Zissimou, Georgia A. Berezin, Andrey A. Koutentis, Panayiotis A. Aldabbagh, Fawaz Molecules Article Cell viability studies for benzo[1,2,4]triazin-7-ones and 1,2,4-benzotriazinyl (Blatter-type) radical precursors are described with comparisons made with 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). All of the stable free radicals were several orders of magnitude less cytotoxic than the benzo[1,2,4]triazin-7-ones. The synthesis and evaluation of two new pyrid-2-yl benzo[1,2,4]triazin-7-ones are described, where altering the 1,3-substitution from phenyl to pyrid-2-yl increased cytotoxicity against most cancer cell lines, as indicated using National Cancer Institute (NCI) one-dose testing. COMPARE analysis of five-dose testing data from the NCI showed very strong correlations to the naturally occurring anti-cancer compound pleurotin. COMPARE is program, which analyzes similarities in cytotoxicity data of compounds, and enables quantitative expression as Pearson correlation coefficients. Compounds were also evaluated using the independent MTT assay, which was compared with SRB assay data generated at the NCI. MDPI 2018-03-03 /pmc/articles/PMC6017941/ /pubmed/29510488 http://dx.doi.org/10.3390/molecules23030574 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Keane, Lee-Ann J. Mirallai, Styliana I. Sweeney, Martin Carty, Michael P. Zissimou, Georgia A. Berezin, Andrey A. Koutentis, Panayiotis A. Aldabbagh, Fawaz Anti-Cancer Activity of Phenyl and Pyrid-2-yl 1,3-Substituted Benzo[1,2,4]triazin-7-ones and Stable Free Radical Precursors |
title | Anti-Cancer Activity of Phenyl and Pyrid-2-yl 1,3-Substituted Benzo[1,2,4]triazin-7-ones and Stable Free Radical Precursors |
title_full | Anti-Cancer Activity of Phenyl and Pyrid-2-yl 1,3-Substituted Benzo[1,2,4]triazin-7-ones and Stable Free Radical Precursors |
title_fullStr | Anti-Cancer Activity of Phenyl and Pyrid-2-yl 1,3-Substituted Benzo[1,2,4]triazin-7-ones and Stable Free Radical Precursors |
title_full_unstemmed | Anti-Cancer Activity of Phenyl and Pyrid-2-yl 1,3-Substituted Benzo[1,2,4]triazin-7-ones and Stable Free Radical Precursors |
title_short | Anti-Cancer Activity of Phenyl and Pyrid-2-yl 1,3-Substituted Benzo[1,2,4]triazin-7-ones and Stable Free Radical Precursors |
title_sort | anti-cancer activity of phenyl and pyrid-2-yl 1,3-substituted benzo[1,2,4]triazin-7-ones and stable free radical precursors |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017941/ https://www.ncbi.nlm.nih.gov/pubmed/29510488 http://dx.doi.org/10.3390/molecules23030574 |
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