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Exploiting the lipophilicity-cytotoxicity relationship of a series of ruthenium(II) complexes to achieve superior cancer cell antiproliferative activity

Haghdoost, Mohammad Mehdi; Golbaghi, Golara; Létourneau, Myriam; Castonguay, Annie . Exploiting the lipophilicity-cytotoxicity relationship of a series of ruthenium(II) complexes to achieve superior cancer cell antiproliferative activity In: Chemistry and Biochem. Graduate Research Conference 2016, 18 Novembre 2016, Montréal (Québec).

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Résumé

Ruthenium complexes are promising candidates to replace platinum-based drugs, as they tend to exhibit high activity against cis-platin resistant cell lines and induce a lower occurrence of side effects than platinum-based complexes, possibly due to their different mechanism of actions [1]. In this study, four new structurally similar Ru(II) complexes with bidentate N,O donor ligands are reported, including the synthesis, characterization and in vitro antiproliferative activity of two different human cancer cell lines, notably MCF-7 (breast) and SH-SY5Y (neuroblastoma). Their structural properties, aquation reactivity, lipophilicity and cellular uptake as well as their ability to catalyze the reduction of NAD+ to NADH under abiotic and biological conditions were also studied. Results showed that the cytotoxicity, cellular uptake and lipophilicity of these complexes are significantly related to each other. The established lipophilicity-cytotoxicity relationship was used to design a ruthenium complex with a much higher antiproliferative activity.

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: 25 juin 2018 14:09
Dernière modification: 25 juin 2018 14:09
URI: http://espace.inrs.ca/id/eprint/5756

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