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Discovery of anti-cancer activity for benzo1,2,4]triazin-7-ones: Very strong correlation to pleurotin and thioredoxin reductase inhibition

dc.contributor.authorSweeney, Martinen
dc.contributor.authorCoyle, Roberten
dc.contributor.authorKavanagh, Paulen
dc.contributor.authorBerezin, Andrey A.en
dc.contributor.authorLo Re, Danieleen
dc.contributor.authorZissimou, Georgia A.en
dc.contributor.authorKoutentis, Panayiotis Andreasen
dc.contributor.authorCarty, Michael P.en
dc.contributor.authorAldabbagh, Fawazen
dc.creatorSweeney, Martinen
dc.creatorCoyle, Roberten
dc.creatorKavanagh, Paulen
dc.creatorBerezin, Andrey A.en
dc.creatorLo Re, Danieleen
dc.creatorZissimou, Georgia A.en
dc.creatorKoutentis, Panayiotis Andreasen
dc.creatorCarty, Michael P.en
dc.creatorAldabbagh, Fawazen
dc.date.accessioned2019-11-21T06:23:04Z
dc.date.available2019-11-21T06:23:04Z
dc.date.issued2016
dc.identifier.urihttp://gnosis.library.ucy.ac.cy/handle/7/56182
dc.source.urihttps://nls.ldls.org.uk/welcome.html?ark:/81055/vdc_100034348639.0x00002a
dc.subjectBiochemistryen
dc.subjectPharmaceutical chemistryen
dc.subjectChemistry, Organicen
dc.subjectBioorganic chemistryen
dc.subjectChemistry, Clinicalen
dc.subjectChimie bio-organiqueen
dc.subjectPériodiquesfr
dc.subjectChimie pharmaceutiquefr
dc.titleDiscovery of anti-cancer activity for benzo1,2,4]triazin-7-ones: Very strong correlation to pleurotin and thioredoxin reductase inhibitionen
dc.typeinfo:eu-repo/semantics/article
dc.author.faculty002 Σχολή Θετικών και Εφαρμοσμένων Επιστημών / Faculty of Pure and Applied Sciences
dc.author.departmentΤμήμα Χημείας / Department of Chemistry
dc.type.uhtypeArticleen
dc.description.notes<p>ID: 1083en
dc.description.notesIn: Bioorganic & medicinal chemistry, Vol. 24, no. 16 ( 2016), p.3565-3570.en
dc.description.notesSummary: Graphical abstractAbstractThe 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.</p>en
dc.contributor.orcidKoutentis, Panayiotis Andreas [0000-0002-4652-7567]
dc.contributor.orcidZissimou, Georgia A. [0000-0003-4821-9469]
dc.gnosis.orcid0000-0002-4652-7567
dc.gnosis.orcid0000-0003-4821-9469


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