CINECA IRIS Institutional Research Information System
IRIS è la soluzione IT che facilita la raccolta e la gestione dei dati relativi alle attività e ai prodotti della ricerca. Fornisce a ricercatori, amministratori e valutatori gli strumenti per monitorare i risultati della ricerca, aumentarne la visibilità e allocare in modo efficace le risorse disponibili.
EnglishWe recently reported the dual (antihormonal and cytotoxic) functionality of ferrocifens, which are organometallic complexes derived from hydroxytamoxifen, the std. mol. in the treatment of hormone-dependent breast cancers. To test the hypothesis that the presence of a ferrocenyl substituent on mols. with an affinity for the estrogen receptor is sufficient to give them cytotoxic properties in vitro, we prepd. complexes derived from estradiol with a ferrocenyl substituent at positions 7α and 17α. The complexes thus obtained retain a satisfactory level of affinity for the estrogen receptor (RBA values higher than 12 %). At low concns. (0.1-1 μM) the complexes show an estrogenic effect in vitro equiv. to that of estradiol on hormone-dependent (MCF-7) breast cancer cells, and no cytotoxic effect on hormone-independent (MDA-MB-231) breast cancer cells. At high concns. (up to 50 μM) the 17α-ethynylferrocenyl estradiol and 7α-ferrocenylmethylthio estradiol become cytotoxic (IC50 = 13.2 μM and 18.8 μM, resp.) while the 17α-ferrocenylestradiol remains non toxic. The low toxicity of these compds. support our hypothesis that electronic communication between the ferrocenyl and phenol moieties in the hydroxyferrocifens series is a key parameter in the generation of cytotoxic effects at submicromolar concns.
| Autori interni: | ||
| Autori: | FIASCHI R; VESSIERES ANNE; SPERA DANIELA; TOP SIDEN; MISTERKIEWICZ BOGUSLAV; HELDT JAN-MARTIN; HILLARD ELIZABETH; HUCHE MICHEL; PLAMONT MARIE-AUDE; NAPOLITANO ELIO: JAOUEN GERARD | |
| Titolo: | The presence of a ferrocenyl unit on an estrogenic molecule is not always sufficient to generate in vitro cytotoxicity | |
| Anno del prodotto: | 2006 | |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
File in questo prodotto:
http://hdl.handle.net/11568/107361
Copyright © 2022