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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

Keane, Lee-Ann, Mirallai, Styliana, Sweeney, Martin, Carty, Michael, Zissimou, Georgia, Berezin, Andrey, Koutentis, Panayiotis 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) , 574. 10.3390/molecules23030574

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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
Date Type: Publication
Status: Published
Schools: Chemistry
Publisher: MDPI
ISSN: 1420-3049
Date of First Compliant Deposit: 20 January 2020
Date of Acceptance: 28 February 2018
Last Modified: 20 Jan 2020 14:00
URI: http://orca-mwe.cf.ac.uk/id/eprint/128753

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