Golbaghi, Golara; Haghdoost, Mohammad Mehdi; Pitard, Irène et Castonguay, Annie 
ORCID: https://orcid.org/0000-0001-5705-6353
.
Multitasking Ru(II) and (III) complexes bearing aromatase inhibitors: synthesis, characterization, in vitro antiproliferative activity and in vivo toxicity assessment
In: 19th Chemistry and Biochem. Graduate Research Conference (CBGRC), 18 Novembre 2016, Montréal, Qc, Canada.
Résumé
Ruthenium complexes are presently an object of great attention in the field of medicinal chemistry, as antitumor agents with selective antimetastatic properties and low systemic toxicity. Interest in Ru anticancer drugs has been growing rapidly since NAMI-A and KP1019 have successfully entered phase II clinical trials. Besides, some ruthenium complexes are active against platinum resistant cells and also display less side effects. Our goal is to create a series of multitasking ruthenium complexes bearing aromatase inhibitors currently used for estrogen receptor positive breast cancer (ER+) therapy. Ruthenium can act as a cell-killing agent through various modes of action, whereas aromatase inhibitors such as Letrozole and Anastrozole can act as anticancer agents by linking to aromatase, blocking the activity of the enzyme responsible for the production of estrogens in postmenopausal women. In this presentation, we report the synthesis of a series of ruthenium-Letrozole and ruthenium-Anastrozole complexes as well as their characterization using various techniques, including nuclear magnetic resonance spectroscopy, X-ray crystallography and high resolution mass spectrometry. In addition, we report their in vitro human breast cancer cell antiproliferative and antimigratory activities, which were assessed by MTS and wound healing assays, respectively. Furthermore, the results of in vivo toxicity test of the complexes on zebrafish embryos are also discussed.
| Type de document: | Document issu d'une conférence ou d'un atelier |
|---|---|
| Informations complémentaires: | Affiche scientifique |
| Mots-clés libres: | - |
| Centre: | Centre INRS-Institut Armand Frappier |
| Date de dépôt: | 30 mars 2018 16:25 |
| Dernière modification: | 21 févr. 2022 17:12 |
| URI: | https://espace.inrs.ca/id/eprint/5745 |
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