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Bipyraloxifene – a modified raloxifene vector against triple-negative breast cancer
dc.creator | Kazimir, Aleksandr | |
dc.creator | Götze, Tom | |
dc.creator | Murganić, Blagoje | |
dc.creator | Mijatović, Sanja | |
dc.creator | Maksimović-Ivanić, Danijela | |
dc.creator | Hey-Hawkins, Evamarie | |
dc.date.accessioned | 2024-07-05T07:56:48Z | |
dc.date.available | 2024-07-05T07:56:48Z | |
dc.date.issued | 2024 | |
dc.identifier.issn | 2632-8682 | |
dc.identifier.uri | http://radar.ibiss.bg.ac.rs/handle/123456789/6853 | |
dc.description.abstract | Raloxifene, a selective oestrogen receptor modulator (SERM), has demonstrated efficacy in the prevention and therapy of oestrogen receptor-positive (ER+) breast cancer, with some degree of effectiveness against triple-negative forms. This suggests the presence of oestrogen receptor-independent pathways in raloxifene-mediated anticancer activity. To enhance the potential of raloxifene against the most aggressive breast cancer cells, hybrid molecules combining the drug with a metal chelator moiety have been developed. In this study, we synthetically modified the structure of raloxifene by incorporating a 2,2′-bipyridine (2,2′-bipy) moiety, resulting in [6-methoxy-2-(4-hydroxyphenyl)benzo[b]thiophen-3-yl]-[4-(2,2′-bipyridin-4′-yl-methoxy)phenyl]methanone (bipyraloxifene). We investigated the cytotoxic activity of both raloxifene and bipyraloxifene against ER+ breast adenocarcinomas, glioblastomas, and a triple-negative breast cancer (TNBC) cell line, elucidating their mode of action against TNBC. Bipyraloxifene maintained a mechanism based on caspase-mediated apoptosis but exhibited significantly higher activity and selectivity compared to the original drug, particularly evident in triple-negative stem-like MDA-MB-231 cells. | sr |
dc.language.iso | en | sr |
dc.publisher | The Royal Society of Chemistry | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/inst-2020/200007/RS// | sr |
dc.relation | DAAD; funding program number: 57440919 | sr |
dc.relation | funding program: Research Grants Bi-national 2019/2021 | sr |
dc.rights | openAccess | sr |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
dc.source | RSC Medicinal Chemistry | sr |
dc.title | Bipyraloxifene – a modified raloxifene vector against triple-negative breast cancer | sr |
dc.type | article | sr |
dc.rights.license | BY | sr |
dc.rights.holder | © The Royal Society of Chemistry 2024 | sr |
dc.citation.issue | 6 | |
dc.citation.volume | 15 | |
dc.identifier.doi | 10.1039/D4MD00051J | |
dc.identifier.scopus | 2-s2.0-85191879221 | |
dc.citation.spage | 1921 | |
dc.citation.epage | 1928 | |
dc.type.version | publishedVersion | sr |
dc.identifier.fulltext | https://radar.ibiss.bg.ac.rs/bitstream/id/18207/d4md00051j.pdf | |
dc.citation.rank | M22~ |