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. and Aldabbagh, Fawaz (2018) Anti-cancer activity of phenyl and pyrid-2-yl 1,3-substituted benzo[1,2,4]triazin-7-ones and stable free radical precursors. Molecules, 23(3), p. 574. ISSN (online) 1420-3049

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Abstract

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.

Item Type: Article
Research Area: Chemistry
Pharmacy
Faculty, School or Research Centre: Faculty of Science, Engineering and Computing (until 2017) > School of Pharmacy and Chemistry
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Depositing User: Fawaz Al-Dabbagh
Date Deposited: 18 Jun 2018 08:37
Last Modified: 13 Jul 2018 13:37
DOI: https://doi.org/10.3390/molecules23030574
URI: http://eprints.kingston.ac.uk/id/eprint/41154

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