Please use this identifier to cite or link to this item: https://hdl.handle.net/11499/9939
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dc.contributor.authorVann, K.R.-
dc.contributor.authorErgün, Y.-
dc.contributor.authorZencir, Sevil-
dc.contributor.authorOncuoglu, S.-
dc.contributor.authorOsheroff, N.-
dc.contributor.authorTopcu, Z.-
dc.date.accessioned2019-08-16T13:07:55Z
dc.date.available2019-08-16T13:07:55Z
dc.date.issued2016-
dc.identifier.issn0960-894X-
dc.identifier.urihttps://hdl.handle.net/11499/9939-
dc.identifier.urihttps://doi.org/10.1016/j.bmcl.2016.02.034-
dc.description.abstractEllipticine (5,11-dimethyl-6H-pyrido[4,3-b]carbazole) is an antineoplastic agent that intercalates into DNA and alters topoisomerase II activity. Unfortunately, this compound displays a number of adverse properties. Therefore, to investigate new ellipticine-based compounds for their potential as topoisomerase II-targeted drugs, we synthesized two novel derivatives, N-methyl-5-demethyl ellipticine (ET-1) and 2-methyl-N-methyl-5-demethyl ellipticinium iodide (ET-2). As determined by DNA decatenation and cleavage assays, ET-1 and ET-2 act as catalytic inhibitors of human topoisomerase II? and are both more potent than the parent compound. Neither compound impairs the ability of the type II enzyme to bind its DNA substrate. Finally, the potency of ET-1 and ET-2 as catalytic inhibitors of topoisomerase II? appears to be related to their ability to intercalate into the double helix. © 2016 Elsevier Ltden_US
dc.language.isoenen_US
dc.publisherElsevier Ltden_US
dc.relation.ispartofBioorganic and Medicinal Chemistry Lettersen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectAnticancer drugsen_US
dc.subjectCatalytic inhibitoren_US
dc.subjectDNA cleavageen_US
dc.subjectDNA intercalationen_US
dc.subjectDNA topoisomerase II?en_US
dc.subjectEllipticine derivativesen_US
dc.subject2 methyl n methyl 5 demethyl ellipticinium iodideen_US
dc.subjectantineoplastic agenten_US
dc.subjectDNA topoisomerase (ATP hydrolysing) Aen_US
dc.subjectellipticineen_US
dc.subjectellipticine derivativeen_US
dc.subjectetoposideen_US
dc.subjectgyrase inhibitoren_US
dc.subjectkinetoplast DNAen_US
dc.subjectn methyl 5 demethyl ellipticineen_US
dc.subjectunclassified drugen_US
dc.subjectDNAen_US
dc.subjectDNA binding proteinen_US
dc.subjectDNA topoisomerase (ATP hydrolysing)en_US
dc.subjectDNA topoisomerase II alphaen_US
dc.subjectintercalating agenten_US
dc.subjecttumor antigenen_US
dc.subjectArticleen_US
dc.subjectcatalysisen_US
dc.subjectcontrolled studyen_US
dc.subjectdrug potencyen_US
dc.subjectdrug protein bindingen_US
dc.subjectdrug synthesisen_US
dc.subjectenzyme activityen_US
dc.subjectenzyme inhibitionen_US
dc.subjecthumanen_US
dc.subjectantagonists and inhibitorsen_US
dc.subjectchemistryen_US
dc.subjectmetabolismen_US
dc.subjectmethylationen_US
dc.subjectAntigens, Neoplasmen_US
dc.subjectDNA Topoisomerases, Type IIen_US
dc.subjectDNA-Binding Proteinsen_US
dc.subjectEllipticinesen_US
dc.subjectHumansen_US
dc.subjectIntercalating Agentsen_US
dc.subjectMethylationen_US
dc.subjectTopoisomerase II Inhibitorsen_US
dc.titleInhibition of human DNA topoisomerase II? by two novel ellipticine derivativesen_US
dc.typeArticleen_US
dc.identifier.volume26en_US
dc.identifier.issue7en_US
dc.identifier.startpage1809
dc.identifier.startpage1809en_US
dc.identifier.endpage1812en_US
dc.identifier.doi10.1016/j.bmcl.2016.02.034-
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.identifier.pmid26906637en_US
dc.identifier.scopus2-s2.0-84979049924en_US
dc.identifier.wosWOS:000371344600033en_US
dc.identifier.scopusqualityQ1-
dc.ownerPamukkale University-
item.languageiso639-1en-
item.fulltextWith Fulltext-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.cerifentitytypePublications-
item.openairetypeArticle-
item.grantfulltextopen-
crisitem.author.dept14.03. Basic Medical Sciences-
Appears in Collections:PubMed İndeksli Yayınlar Koleksiyonu / PubMed Indexed Publications Collection
Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
Tıp Fakültesi Koleksiyonu
WoS İndeksli Yayınlar Koleksiyonu / WoS Indexed Publications Collection
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