- Titel
- Bipyraloxifene – a modified raloxifene vector against triple-negative breast cancer
- Zitierfähige Url:
- https://nbn-resolving.org/urn:nbn:de:bsz:15-qucosa2-1021348
- Quellenangabe
- RSC Medicinal Chemistry
Erscheinungsjahr: 2024
Jahrgang: 15
Heft: 6
Seiten: 1921-1928
E-ISSN: 2632-8682 - Erstveröffentlichung
- 2024
- Abstract (EN)
- 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.
- Andere Ausgabe
- Erstveröffentlichung
DOI: 10.1039/d4md00051j - Freie Schlagwörter (EN)
- Bipyraloxifene, breast cancer, triple-negative breast cancer, raloxifene vector
- Klassifikation (DDC)
- 540
- Verlag
- The Royal Society of Chemistry, London
- Förder- / Projektangaben
- Deutscher Akademischer Austauschdienst (DAAD)
ID: 57440919 - Version / Begutachtungsstatus
- publizierte Version / Verlagsversion
- URN Qucosa
- urn:nbn:de:bsz:15-qucosa2-1021348
- Veröffentlichungsdatum Qucosa
- 06.02.2026
- Dokumenttyp
- Artikel
- Sprache des Dokumentes
- Englisch
- Lizenz / Rechtehinweis
CC BY 4.0