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Exploring the potential of tamoxifen-based copper(II) dichloride in breast cancer therapy
dc.creator | Kazimir, Aleksandr | |
dc.creator | Schwarze, Benedikt | |
dc.creator | Lönnecke, Peter | |
dc.creator | Jelača, Sanja | |
dc.creator | Mijatović, Sanja | |
dc.creator | Maksimović-Ivanić, Danijela | |
dc.creator | Hey-Hawkins, Evamarie | |
dc.date.accessioned | 2023-11-08T13:53:06Z | |
dc.date.available | 2023-11-08T13:53:06Z | |
dc.date.issued | 2023 | |
dc.identifier.issn | 2632-8682 | |
dc.identifier.uri | http://radar.ibiss.bg.ac.rs/handle/123456789/6266 | |
dc.description.abstract | For decades, tamoxifen-based hormone therapy has effectively addressed oestrogen receptor positive (ER+) luminal A breast cancer. Nonetheless, the emergence of tamoxifen resistance required innovative approaches, leading to hybrid metallodrugs with several therapeutic effects besides the inhibition of oestrogen receptor α (ERα). Drawing inspiration from tamoxifen metabolite structures (4-hydroxytamoxifen and 4,4′-dihyroxytamoxifen), a phenyl ring was replaced by a bidentate 2,2′-bipyridine donor moiety to give 4-[1,1-bis(4-methoxyphenyl)but-1-en-2-yl]-2,2′-bipyridine (L), enabling coordination of bioactive transition metal compounds such as copper(II) dichloride, yielding [CuCl(μ-Cl)(L-κ2N,N′)]2 (1). Notably, copper(II) complex 1 exhibited remarkable activity within the low micromolar concentration range against ER+ human glioblastoma U251, as well as breast carcinomas MDA-MB-361 and MCF-7, surpassing the efficacy of previously reported palladium(II) and platinum(II) dichloride analogs against these cell lines. The pronounced efficacy of complex 1 against triple-negative MDA-MB-231 cells highlights its potential multitherapeutic approach, evident through induction of apoptosis and antioxidant activity. This study evaluates the potential of copper–tamoxifen hybrid complex 1 as a potent therapeutic candidate, highlighting its diverse mechanism of action against challenging breast cancer subtypes. | sr |
dc.language.iso | en | sr |
dc.publisher | Royal Society of Chemistry | sr |
dc.relation | DAAD funding (funding program number: 57440919; funding program: Research Grants – Bi-national 2019/2020) | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/inst-2020/200007/RS// | sr |
dc.rights | openAccess | sr |
dc.rights.uri | https://creativecommons.org/licenses/by-nc/4.0/ | |
dc.source | RSC Medicinal Chemistry | sr |
dc.title | Exploring the potential of tamoxifen-based copper(II) dichloride in breast cancer therapy | sr |
dc.type | article | sr |
dc.rights.license | BY-NC | sr |
dc.rights.holder | © The Royal Society of Chemistry 2023 | sr |
dc.identifier.doi | 10.1039/d3md00344b | |
dc.identifier.scopus | 2-s2.0-85174334318 | |
dc.citation.apa | Kazimir, Aleksandr, Benedikt Schwarze, Peter Lönnecke, Sanja Jelača, Sanja Mijatovic, Danijela Maksimovic-Ivanic, and Evamarie Hey-Hawkins. 2023. “Exploring the Potential of Tamoxifen-Based Copper(II) Dichloride in Breast Cancer Therapy.” RSC Medicinal Chemistry. | |
dc.citation.vancouver | Kazimir A, Schwarze B, Lönnecke P, Jelača S, Mijatovic S, Maksimovic-Ivanic D, Hey-Hawkins E. Exploring the Potential of Tamoxifen-based Copper(II) Dichloride in Breast Cancer Therapy. RSC Med Chem. 2023; | |
dc.type.version | publishedVersion | sr |
dc.identifier.fulltext | https://radar.ibiss.bg.ac.rs/bitstream/id/15482/bitstream_15482.pdf | |
dc.citation.rank | M22~ |