Show simple item record

dc.creatorJeremić, Marko
dc.creatorPešić, Milica
dc.creatorDinić, Jelena
dc.creatorBankovic, Jasna
dc.creatorNovaković, Irena
dc.creatorŠegan, Dejan
dc.creatorSladić, Dušan
dc.date.accessioned2019-01-30T17:48:30Z
dc.date.available2019-01-30T17:48:30Z
dc.date.issued2016
dc.identifier.issn0223-5234
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/1862
dc.description.abstractIn this work, synthesis of alkylamino and aralkylamino derivatives of sesquiterpene quinone avarone and its model compound tert-butylquinone was described. For all obtained derivatives biological activity was studied. Cytotoxic activity of the synthesized derivatives towards multidrug resistant MDR human non small cell lung carcinoma NCI-H460/R cells, their sensitive counterpart NCI-H460 and human normal keratinocytes (HaCaT) as well as detection of cell death superoxide anion generation were investigated. Antimicrobial activity towards Gram positive and Gram negative bacteria and fungal cultures was determined. The results showed that strong cytotoxic activity toward cancer cells was improved with simple avarone mimetics. Some derivatives were selective towards MDR cancer cells. The most active derivatives induced apoptosis in both cancer cell lines, but not in normal cells. Superoxide production was induced by 2,6-disubstituted compounds in MDR cancer cells and not by less active 2,5-disubstituted compounds and was accompanied by the collapse of the mitochondrial transmembrane potential. Two tert-butylquinone derivatives were particularly selective towards MDR cancer cells. Some tert-butylquinone derivatives exhibited a strong antimicrobial activity.en
dc.publisherElsevier France-Editions Scientifiques Medicales Elsevier, Paris
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172055/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/41031/RS//
dc.rightsrestrictedAccess
dc.sourceEuropean Journal of Medicinal Chemistry
dc.subjectQuinonesen
dc.subjectAnticancer activityen
dc.subjectMultidrug resistanten
dc.subjectApoptosisen
dc.subjectROS generationen
dc.subjectMitochondrial potentialen
dc.titleSimple avarone mimetics as selective agents against multidrug resistant cancer cellsen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractСеган, Дејан; Диниц, Јелена; Јеремиц, Марко; Новаковић, Ирена; Сладиц, Дуган; Песиц, Милица; Банковиц, Јасна;
dc.citation.volume118
dc.citation.spage107
dc.citation.epage120
dc.citation.other118: 107-120
dc.citation.rankaM21
dc.identifier.pmid27128177
dc.identifier.doi10.1016/j.ejmech.2016.04.011
dc.identifier.rcubConv_3553
dc.identifier.scopus2-s2.0-84964477857
dc.identifier.wos000377312400011
dc.type.versionpublishedVersion


Files in this item

Thumbnail

This item appears in the following Collection(s)

Show simple item record