dc.contributor.author | Sweeney, M. | en |
dc.contributor.author | Coyle, R. | en |
dc.contributor.author | Kavanagh, P. | en |
dc.contributor.author | Berezin, Andrey A. | en |
dc.contributor.author | Lo Re, D. | en |
dc.contributor.author | Zissimou, Georgia A. | en |
dc.contributor.author | Koutentis, Panayiotis Andreas | en |
dc.contributor.author | Carty, Michael P. | en |
dc.contributor.author | Aldabbagh, Fawaz | en |
dc.creator | Sweeney, M. | en |
dc.creator | Coyle, R. | en |
dc.creator | Kavanagh, P. | en |
dc.creator | Berezin, Andrey A. | en |
dc.creator | Lo Re, D. | en |
dc.creator | Zissimou, Georgia A. | en |
dc.creator | Koutentis, Panayiotis Andreas | en |
dc.creator | Carty, Michael P. | en |
dc.creator | Aldabbagh, Fawaz | en |
dc.date.accessioned | 2019-11-21T06:23:04Z | |
dc.date.available | 2019-11-21T06:23:04Z | |
dc.date.issued | 2016 | |
dc.identifier.uri | http://gnosis.library.ucy.ac.cy/handle/7/56181 | |
dc.description.abstract | The thioredoxin (Trx)–thioredoxin reductase (TrxR) system plays a key role in maintaining the cellular redox balance with Trx being over-expressed in a number of cancers. Inhibition of TrxR is an important strategy for anti-cancer drug discovery. The natural product pleurotin is a well-known irreversible inhibitor of TrxR. The cytotoxicity data for benzo[1,2,4]triazin-7-ones showed very strong correlation (Pearson correlation coefficients ∼0.8) to pleurotin using National Cancer Institute COMPARE analysis. A new 3-CF3substituted benzo[1,2,4]triazin-7-one gave submicromolar inhibition of TrxR, although the parent compound 1,3-diphenylbenzo[1,2,4]triazin-7-one was more cytotoxic against cancer cell lines. Benzo[1,2,4]triazin-7-ones exhibited different types of reversible inhibition of TrxR, and cyclic voltammetry showed characteristic quasi-reversible redox processes. Cell viability studies indicated strong dependence of cytotoxicity on substitution at the 6-position of the 1,3-diphenylbenzo[1,2,4]triazin-7-one ring. © 2016 Elsevier Ltd | en |
dc.source | Bioorganic and Medicinal Chemistry | en |
dc.source.uri | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84973558703&doi=10.1016%2fj.bmc.2016.05.066&partnerID=40&md5=f6ca1b43c6859ffcc543f663f81b75fd | |
dc.subject | antineoplastic agent | en |
dc.subject | Antineoplastic Agents | en |
dc.subject | human | en |
dc.subject | Humans | en |
dc.subject | controlled study | en |
dc.subject | unclassified drug | en |
dc.subject | Article | en |
dc.subject | drug screening | en |
dc.subject | human cell | en |
dc.subject | chemistry | en |
dc.subject | drug cytotoxicity | en |
dc.subject | enzyme inhibition | en |
dc.subject | drug synthesis | en |
dc.subject | oxidation reduction reaction | en |
dc.subject | drug development | en |
dc.subject | antagonists and inhibitors | en |
dc.subject | Drug Screening Assays, Antitumor | en |
dc.subject | Drug Discovery | en |
dc.subject | cyclic potentiometry | en |
dc.subject | triazine derivative | en |
dc.subject | 1,2,4 benzotriazine derivative | en |
dc.subject | Triazines | en |
dc.subject | 1 phenyl 3 (trifluoromethyl)benzo[1,2,4]triazin 7 one | en |
dc.subject | 1,3 diphenyl 6 (piperidin 1 yl)benzo[1,2,4]triazin 7 one | en |
dc.subject | 1,3 diphenyl 6 (pyrrolidin 1 yl)benzo[1,2,4]triazin 7 one | en |
dc.subject | 1,3 diphenyl 6 thiomorpholinobenzo[1,2,4]triazin 7 one | en |
dc.subject | 1,3 diphenylbenzo[1,2,4]triazin 7 one | en |
dc.subject | 6 (diethylamino) 1,3 diphenylbenzo[1,2,4]triazin 7 one | en |
dc.subject | 6 (ethylamino) 1,3 diphenylbenzo[1,2,4]triazin 7 one | en |
dc.subject | 6 (methylamino) 1,3 diphenylbenzo[1,2,4]triazin 7 one | en |
dc.subject | 6 amino 1,3 diphenylbenzo[1,2,4]triazin 7 one | en |
dc.subject | 6 ethoxy 1,3 diphenylbenzo[1,2,4]triazin 7 one | en |
dc.subject | 6 methoxy 1,3 diphenylbenzo[1,2,4]triazin 7 one | en |
dc.subject | 6 morpholino 1,3 diphenylbenzo[1,2,4]triazin 7 one | en |
dc.subject | anthracene derivative | en |
dc.subject | Anti-tumor | en |
dc.subject | benzo[1,2,4]triazin 7 one derivative | en |
dc.subject | Bioreduction | en |
dc.subject | cancer cell line | en |
dc.subject | Cell Line, Transformed | en |
dc.subject | fused heterocyclic rings | en |
dc.subject | Heterocyclic compound | en |
dc.subject | Heterocyclic Compounds, 4 or More Rings | en |
dc.subject | matrix-assisted laser desorption-ionization mass spectrometry | en |
dc.subject | MTT assay | en |
dc.subject | n (7 oxo 1,3 diphenyl 1,7 dihydrobenzo[1,2,4]triazin 6 yl)acetamide | en |
dc.subject | NCI-DTP COMPARE program | en |
dc.subject | pleurotin | en |
dc.subject | Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization | en |
dc.subject | thioredoxin reductase | en |
dc.subject | Thioredoxin-Disulfide Reductase | en |
dc.subject | transformed cell line | en |
dc.title | Discovery of anti-cancer activity for benzo[1,2,4]triazin-7-ones: Very strong correlation to pleurotin and thioredoxin reductase inhibition | en |
dc.type | info:eu-repo/semantics/article | |
dc.identifier.doi | 10.1016/j.bmc.2016.05.066 | |
dc.description.volume | 24 | |
dc.description.issue | 16 | |
dc.description.startingpage | 3565 | |
dc.description.endingpage | 3570 | |
dc.author.faculty | 002 Σχολή Θετικών και Εφαρμοσμένων Επιστημών / Faculty of Pure and Applied Sciences | |
dc.author.department | Τμήμα Χημείας / Department of Chemistry | |
dc.type.uhtype | Article | en |
dc.description.notes | <p>Cited By :1</p> | en |
dc.source.abbreviation | Bioorg.Med.Chem. | en |
dc.contributor.orcid | Koutentis, Panayiotis Andreas [0000-0002-4652-7567] | |
dc.contributor.orcid | Zissimou, Georgia A. [0000-0003-4821-9469] | |
dc.gnosis.orcid | 0000-0002-4652-7567 | |
dc.gnosis.orcid | 0000-0003-4821-9469 | |