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Exploring Raloxifene-based Metallodrugs: A Versatile Vector Combined with Pt(II), Palladium(II) and Nickel(II) Dichlorides and Carborates against Triple-Negative Breast Cancer
dc.creator | Kazimir, Aleksandr | |
dc.creator | Götze, Tom | |
dc.creator | Lönnecke, Peter | |
dc.creator | Murganić, Blagoje | |
dc.creator | Mijatović, Sanja | |
dc.creator | Maksimović-Ivanić, Danijela | |
dc.creator | Hey-Hawkins, Evamarie | |
dc.date.accessioned | 2024-07-04T10:14:55Z | |
dc.date.available | 2024-07-04T10:14:55Z | |
dc.date.issued | 2024 | |
dc.identifier.issn | 1860-7179 | |
dc.identifier.uri | http://radar.ibiss.bg.ac.rs/handle/123456789/6851 | |
dc.description.abstract | Triple-negative breast cancer (TNBC) poses challenges in therapy due to the absence of target expression such as estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor receptor 2 (HER2). Frequently, the treatment of TNBC involves the combination of several therapeutics. However, an enhanced therapeutic effect can be also achieved within a single molecule. The efficacy of raloxifene can be improved by designing a raloxifene-based hybrid drug bearing a 2,2’-bipyridine moiety (2). Integration of platinum(II), palladium(II), and nickel(II) complexes into this structure dramatically changed the cytotoxicity. The platinum(II) dichloride complex 3 did not demonstrate any activity, while palladium(II) and nickel(II) dichloride complexes 4 and 5 exhibited various cytotoxic behavior towards different types of hormone-receptor positive (HR+) cancer and TNBC cell lines. The replacement of the two chlorido ligands in 3‒5 with a dicarbollide (carborate) ion [C2B9H11]2- resulted in reduced activity of compounds 6, 7, and 8. However, the palladacarborane complex 7 demonstrated higher selectivity towards TNBC. Furthermore, the mechanism of action was shifted from cytotoxic to explicitly cytostatic with detectable proliferation arrest and accelerated aging, characterized by senescence-associated phenotype of TNBC cells. This study provides valuable insights into the development of hybrid therapeutics against TNBC. | sr |
dc.language.iso | en | sr |
dc.publisher | John Wiley and Sons | 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 2019/2020 | sr |
dc.rights | openAccess | sr |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/4.0/ | |
dc.source | ChemMedChem | sr |
dc.subject | TNBC | sr |
dc.subject | group 10 metals | sr |
dc.subject | metallacarborane | sr |
dc.subject | metallodrugs | sr |
dc.subject | raloxifene | sr |
dc.title | Exploring Raloxifene-based Metallodrugs: A Versatile Vector Combined with Pt(II), Palladium(II) and Nickel(II) Dichlorides and Carborates against Triple-Negative Breast Cancer | sr |
dc.type | article | sr |
dc.rights.license | BY-NC-ND | sr |
dc.rights.holder | © 2024 The Authors. ChemMedChem published by Wiley-VCH GmbH | sr |
dc.identifier.doi | 10.1002/cmdc.202400006 | |
dc.identifier.pmid | 38642018 | |
dc.identifier.scopus | 2-s2.0-85195165225 | |
dc.identifier.wos | 001238902600001 | |
dc.citation.spage | e202400006 | |
dc.type.version | publishedVersion | sr |
dc.identifier.fulltext | https://radar.ibiss.bg.ac.rs/bitstream/id/18188/bitstream_18188.pdf | |
dc.citation.rank | M22~ |