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dc.creatorFilipović, Nenad
dc.creatorBjelogrlić, Snežana
dc.creatorPelliccia, Sveva
dc.creatorJovanović, Vesna B.
dc.creatorKojić, Milan
dc.creatorSencanski, Milan
dc.creatorLa Regina, Giuseppe
dc.creatorSilvestri, Romano
dc.creatorMuller, Christian D.
dc.creatorTodorović, Tamara R.
dc.date.accessioned2020-12-17T22:56:04Z
dc.date.available2020-12-17T22:56:04Z
dc.date.issued2020
dc.identifier.issn1878-5352
dc.identifier.urihttp://aspace.agrif.bg.ac.rs/handle/123456789/5364
dc.description.abstractTriapine, the most studied alpha-N-heterocyclic thiosemicarbazone, revealed potent activity against advanced leukemia, but was ineffective against a variety of solid tumors. Moreover, methemoglobinemia, which is a side effect of triapine administration, may limits all clinical application. To enhance anticancer activity and reduce side effects, we applied an isosteric replacement of sulfur to selenium atom was performed by synthesis and characterization of selenium triapine analog, 3-aminopyridine-2-carboxaldehyde selenosemicarbazone (selenotriapine). Compared to triapine, selenotriapine revealed superior pro-apoptotic activity with activation of intrinsic apoptotic pathway in both human monocytic leukemia (THP-1) and mammary adenocarcinoma (MCF-7) cell lines. For MCF-7 2-D cultures, selenotriapine induced notable increase in mitochondrial superoxide radical generation and dissipation of mitochondrial transmembrane potential. A significant delay in growth of MCF-7 spheroids (3-D culture) was accompanied by phenotypic stem cell reprogramming (Oct-4 expression). Additionally, selenotriapine demonstrated a very low toxicity profile as compared to triapine, confirmed over alleviated extent of methemoglobin formation and higher IC50 value in brine shrimp cytotoxicity assay.en
dc.publisherElsevier, Amsterdam
dc.relationCOSTEuropean Cooperation in Science and Technology (COST) [CA15135, CA16119]
dc.relationPRIN 2015Ministry of Education, Universities and Research (MIUR)Research Projects of National Relevance (PRIN) [2015FCHJ8E]
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172055/RS//
dc.rightsopenAccess
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/4.0/
dc.sourceArabian Journal of Chemistry
dc.subjectSelenosemicarbazoneen
dc.subject3-D cultureen
dc.subjectApoptosisen
dc.subjectMitochondrial superoxide productionen
dc.subjectOct-4en
dc.titleSelenotriapine - An isostere of the most studied thiosemicarbazone with pronounced pro-apoptotic activity, low toxicity and ability to challenge phenotype reprogramming of 3-D mammary adenocarcinoma tumorsen
dc.typearticle
dc.rights.licenseBY-NC-ND
dc.citation.epage1489
dc.citation.issue1
dc.citation.other13(1): 1466-1489
dc.citation.rankM21
dc.citation.spage1466
dc.citation.volume13
dc.identifier.doi10.1016/j.arabjc.2017.11.017
dc.identifier.fulltexthttp://aspace.agrif.bg.ac.rs/bitstream/id/3861/5361.pdf
dc.identifier.scopus2-s2.0-85037552505
dc.identifier.wos000505076000109
dc.type.versionpublishedVersion


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