dc.creator | Jeremić, Marko | |
dc.creator | Pešić, Milica | |
dc.creator | Dinić, Jelena | |
dc.creator | Bankovic, Jasna | |
dc.creator | Novaković, Irena | |
dc.creator | Šegan, Dejan | |
dc.creator | Sladić, Dušan | |
dc.date.accessioned | 2021-05-10T15:15:17Z | |
dc.date.available | 2021-05-10T15:15:17Z | |
dc.date.issued | 2016 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/4580 | |
dc.description.abstract | In 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.publisher | Elsevier France-Editions Scientifiques Medicales Elsevier, Paris | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172055/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/41031/RS// | |
dc.relation.isreferencedby | https://doi.org/10.1016/j.ejmech.2016.04.011 | |
dc.relation.isreferencedby | https://cer.ihtm.bg.ac.rs/handle/123456789/1862 | |
dc.relation.isreferencedby | https://cer.ihtm.bg.ac.rs/handle/123456789/4579 | |
dc.rights | openAccess | |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
dc.source | European Journal of Medicinal Chemistry | |
dc.subject | Quinones | en |
dc.subject | Anticancer activity | en |
dc.subject | Multidrug resistant | en |
dc.subject | Apoptosis | en |
dc.subject | ROS generation | en |
dc.subject | Mitochondrial potential | en |
dc.title | Supplementary material for: "Simple avarone mimetics as selective agents against multidrug resistant cancer cells" | en |
dc.type | dataset | |
dc.rights.license | BY | |
dcterms.abstract | Јеремић, Марко; Динић, Јелена; Банковиц, Јасна; Новаковић, Ирена; Шеган, Дејан; Сладић, Душан; Пешић, Милица; | |
dc.description.other | The supplementary material for: Jeremić, M., Pešić, M., Dinić, J., Bankovic, J., Novaković, I., Šegan, D.,& Sladić, D. (2016). Simple avarone mimetics as selective agents against multidrug resistant cancer cells. European Journal of Medicinal Chemistry, 118, 107-120. [https://doi.org/10.1016/j.ejmech.2016.04.011] | |
dc.description.other | Published version of the aticle: [https://cer.ihtm.bg.ac.rs/handle/123456789/1862] | |
dc.description.other | The peer-reviewed version of the article: [https://cer.ihtm.bg.ac.rs/handle/123456789/4579] | |
dc.identifier.rcub | https://hdl.handle.net/21.15107/rcub_cer_4580 | |
dc.identifier.fulltext | https://cer.ihtm.bg.ac.rs/bitstream/id/20237/si-s2-0-S0223523416302938-mmc1.pdf | |
dc.type.version | publishedVersion | |