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Article

Anti-Cancer Activity of Phenyl and Pyrid-2-yl 1,3-Substituted Benzo[1,2,4]triazin-7-ones and Stable Free Radical Precursors

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School of Chemistry, National University of Ireland Galway, University Road, H91 TK3 Galway, Ireland
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Biochemistry, School of Natural Sciences, National University of Ireland Galway, University Road, H91 TK33 Galway, Ireland
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Department of Chemistry, University of Cyprus, P.O. Box 20537, Nicosia 1678, Cyprus
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Department of Pharmacy, School of Life Sciences, Pharmacy and Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames, KT1 2EE, UK
*
Author to whom correspondence should be addressed.
Molecules 2018, 23(3), 574; https://doi.org/10.3390/molecules23030574
Received: 6 February 2018 / Revised: 26 February 2018 / Accepted: 28 February 2018 / Published: 3 March 2018
(This article belongs to the Section Medicinal Chemistry)
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. View Full-Text
Keywords: anti-tumour; blatter-type radical; heterocyclic compound; NCI; pleurotin; TEMPO anti-tumour; blatter-type radical; heterocyclic compound; NCI; pleurotin; TEMPO
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MDPI and ACS Style

Keane, L.-A.J.; Mirallai, S.I.; Sweeney, M.; Carty, M.P.; Zissimou, G.A.; Berezin, A.A.; Koutentis, P.A.; Aldabbagh, F. 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 2018, 23, 574. https://doi.org/10.3390/molecules23030574

AMA Style

Keane L-AJ, Mirallai SI, Sweeney M, Carty MP, Zissimou GA, Berezin AA, Koutentis PA, Aldabbagh F. 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. 2018; 23(3):574. https://doi.org/10.3390/molecules23030574

Chicago/Turabian Style

Keane, Lee-Ann J., Styliana I. Mirallai, Martin Sweeney, Michael P. Carty, Georgia A. Zissimou, Andrey A. Berezin, Panayiotis A. Koutentis, and Fawaz Aldabbagh. 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, no. 3: 574. https://doi.org/10.3390/molecules23030574

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