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 Mirallai, Styliana Sweeney, Martin Carty, Michael Zissimou, Georgia Berezin, Andrey Koutentis, Panayiotis Aldabbagh, Fawaz
Keane, Lee-Ann
Mirallai, Styliana
Sweeney, Martin
Carty, Michael
Zissimou, Georgia
Berezin, Andrey
Koutentis, Panayiotis
Aldabbagh, Fawaz
Publication Date
2018-03-03
Type
Article
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Citation
Keane, Lee-Ann; Mirallai, Styliana; Sweeney, Martin; Carty, Michael; Zissimou, Georgia; Berezin, Andrey; Koutentis, Panayiotis; 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),
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.
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Publisher
MDPI AG
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Attribution-NonCommercial-NoDerivs 3.0 Ireland