Golbaghi, Golara; Haghdoost, Mohammad Mehdi; Yancu, Debbie; Lopez de los Santos, Yossef; Doucet, Nicolas 
ORCID: https://orcid.org/0000-0002-1952-9380; Patten, Shunmoogum A.; Sanderson, J. Thomas ORCID: https://orcid.org/0000-0002-3190-2811 et Castonguay, Annie ORCID: https://orcid.org/0000-0001-5705-6353
(2019).
Organoruthenium(II) Complexes Bearing an Aromatase Inhibitor: Synthesis, Characterization, in Vitro Biological Activity and in Vivo Toxicity in Zebrafish Embryos
Organometallics
, vol. 38
, nº 3.
pp. 702-711.
DOI: 10.1021/acs.organomet.8b00897.
Résumé
Some symbols could not be reproduce. For the full abstract, see the original article.
Third-generation aromatase inhibitors such as anastrozole (ATZ) and letrozole (LTZ) are widely used to treat estrogen receptor-positive (ER+) breast cancers in postmenopausal women. Investigating their ability to coordinate metals could lead to the emergence of a new category of anticancer drug candidates with a broader spectrum of pharmacological activities. In this study, a series of ruthenium(II) arene complexes bearing the aromatase inhibitor anastrozole was synthesized and characterized. Among these complexes, [Ru(η6-C6H6)(PPh3)(η1-ATZ)Cl]BPh4 (3) was found to be the most stable in cell culture media, to lead to the highest cellular uptake and in vitro cytotoxicity in two ER+ human breast cancer cell lines (MCF7 and T47D), and to induce a decrease in aromatase activity in H295R cells. Exposure of zebrafish embryos to complex 3 (12.5 μM) did not lead to noticeable signs of toxicity over 96 h, making it a suitable candidate for further in vivo investigations.
| Type de document: | Article |
|---|---|
| Mots-clés libres: | - |
| Centre: | Centre INRS-Institut Armand Frappier |
| Date de dépôt: | 07 août 2019 13:48 |
| Dernière modification: | 15 févr. 2022 15:33 |
| URI: | https://espace.inrs.ca/id/eprint/8115 |
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