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...
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MDPI AG
2018-03-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/23/3/574 |
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doaj-36f4cdc6199b44dcbc1b0fac811328212020-11-24T22:43:11ZengMDPI AGMolecules1420-30492018-03-0123357410.3390/molecules23030574molecules23030574Anti-Cancer Activity of Phenyl and Pyrid-2-yl 1,3-Substituted Benzo[1,2,4]triazin-7-ones and Stable Free Radical PrecursorsLee-Ann J. Keane0Styliana I. Mirallai1Martin Sweeney2Michael P. Carty3Georgia A. Zissimou4Andrey A. Berezin5Panayiotis A. Koutentis6Fawaz Aldabbagh7School of Chemistry, National University of Ireland Galway, University Road, H91 TK3 Galway, IrelandSchool of Chemistry, National University of Ireland Galway, University Road, H91 TK3 Galway, IrelandSchool of Chemistry, National University of Ireland Galway, University Road, H91 TK3 Galway, IrelandBiochemistry, School of Natural Sciences, National University of Ireland Galway, University Road, H91 TK33 Galway, IrelandDepartment of Chemistry, University of Cyprus, P.O. Box 20537, Nicosia 1678, CyprusDepartment of Chemistry, University of Cyprus, P.O. Box 20537, Nicosia 1678, CyprusDepartment of Chemistry, University of Cyprus, P.O. Box 20537, Nicosia 1678, CyprusSchool of Chemistry, National University of Ireland Galway, University Road, H91 TK3 Galway, IrelandCell 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.http://www.mdpi.com/1420-3049/23/3/574anti-tumourblatter-type radicalheterocyclic compoundNCIpleurotinTEMPO |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Lee-Ann J. Keane Styliana I. Mirallai Martin Sweeney Michael P. Carty Georgia A. Zissimou Andrey A. Berezin Panayiotis A. Koutentis Fawaz Aldabbagh |
| spellingShingle |
Lee-Ann J. Keane Styliana I. Mirallai Martin Sweeney Michael P. Carty Georgia A. Zissimou Andrey A. Berezin Panayiotis A. Koutentis Fawaz Aldabbagh 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 anti-tumour blatter-type radical heterocyclic compound NCI pleurotin TEMPO |
| author_facet |
Lee-Ann J. Keane Styliana I. Mirallai Martin Sweeney Michael P. Carty Georgia A. Zissimou Andrey A. Berezin Panayiotis A. Koutentis Fawaz Aldabbagh |
| author_sort |
Lee-Ann J. Keane |
| 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_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_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_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 |
| publisher |
MDPI AG |
| series |
Molecules |
| issn |
1420-3049 |
| publishDate |
2018-03-01 |
| 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. |
| topic |
anti-tumour blatter-type radical heterocyclic compound NCI pleurotin TEMPO |
| url |
http://www.mdpi.com/1420-3049/23/3/574 |
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