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dc.creatorElshaflu, Hana
dc.creatorTodorović, Tamara
dc.creatorNikolić, Milan
dc.creatorLolic, Aleksandar
dc.creatorVišnjevac, Aleksandar
dc.creatorHagenow, Stefanie
dc.creatorPadron, Jose M.
dc.creatorGarcia-Sosa, Alfonso T.
dc.creatorĐorđević, Ivana
dc.creatorGrubišić, Sonja
dc.creatorStark, Holger
dc.creatorFilipovic, Nenad R.
dc.date.accessioned2019-01-30T18:00:37Z
dc.date.available2019-01-30T18:00:37Z
dc.date.issued2018
dc.identifier.issn2296-2646
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/2443
dc.description.abstractThe novel approach in the treatment of complex multifactorial diseases, such as neurodegenerative disorders and cancer, requires a development of efficient multi-targeting oriented drugs. Since oxidative stress significantly contributes to the pathogenesis of cancer and neurodegenerative disorders, potential drug candidates should possess good antioxidant properties Due to promising biological activities shown for structurally related (1,3-thiazol-2-yl)hydrazones, a focused library of 12 structurally related benzylidene-based (1,3-selenazol-2-yl)hydrazones was designed as potential multi-targeting compounds. Monoamine oxidases (MAO) A/B inhibition properties of this class of compounds have been investigated. Surprisingly, the p-nitrophenyl-substituted (1,3-selenazol-2-yl)hydrazone 4 showed MAO B inhibition in a nanomolar concentration range (IC50 = 73 nM). Excellent antioxidant properties were confirmed in a number of different in vitro assays. Antiproliferative activity screening on a panel of six human solid tumor cell lines showed that potencies of some of the investigated compounds was comparable or even better than that of the positive control 5-fluorouracil. In-silico calculations of ADME properties pointed to promising good pharmacokinetic profiles of investigated compounds. Docking studies suggest that some compounds, compared to positive controls, have the ability to strongly interact with targets relevant to cancer such as 5'-nucleotidase, and to neurodegenerative diseases such as the small conductance calcium-activated potassium channel protein 1, in addition to confirmation of inhibitory binding at MAO B.en
dc.publisherFrontiers Media Sa, Lausanne
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172055/RS//
dc.relationGerman Research Foundation (DFG) [INST 208/664-1 FUGG]
dc.relationCOST Action [CA15135]
dc.relationEstonian Ministry for Education and Research [IUT34-14]
dc.rightsopenAccess
dc.sourceFrontiers in Chemistry
dc.subjectselenazolesen
dc.subjectMAO Ben
dc.subjectAnticancer activityen
dc.subjectDockingen
dc.subjectAntioxidant agentsen
dc.titleSelenazolyl-hydrazones as Novel Selective MAO Inhibitors With Antiproliferative and Antioxidant Activities: Experimental and In-silico Studiesen
dc.typearticle
dc.rights.licenseBY
dcterms.abstractТодоровиц, Тамара Р.; Филиповиц, Ненад Р.; Ђорђевић, Ивана; Грубишић, Соња; Лолиц, Aлександар; Николиц, Милан; Хагеноw, Стефание; Падрон, Јосе М.; Старк, Холгер; Елсхафлу, Хана; Висњевац, Aлександар; Гарциа-Соса, Aлфонсо Т.;
dc.citation.volume6
dc.citation.other6:
dc.citation.rankM21
dc.identifier.pmid30018949
dc.identifier.doi10.3389/fchem.2018.00247
dc.identifier.rcubConv_3962
dc.identifier.fulltexthttp://cer.ihtm.bg.ac.rs//bitstream/id/8802/2441.pdf
dc.identifier.scopus2-s2.0-85053084992
dc.identifier.wos000437129200001
dc.type.versionpublishedVersion


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