Côrte-Real, LeonorKaras, BrittanyGírio, PatríciaMoreno, AlexisAvecilla, FernandoMarques, FernandaBuckley, Brian T.Cooper, Keith R.Doherty, CathleenFalson, PierreGarcia, Maria HelenaValente, Andreia2025-01-132025-01-132019-02-01Leonor Côrte-Real, Brittany Karas, Patrícia Gírio, Alexis Moreno, Fernando Avecilla, Fernanda Marques, Brian T. Buckley, Keith R. Cooper, Cathleen Doherty, Pierre Falson, M. Helena Garcia, Andreia Valente, Unprecedented inhibition of P-gp activity by a novel ruthenium-cyclopentadienyl compound bearing a bipyridine-biotin ligand, European Journal of Medicinal Chemistry, Volume 163, 2019, Pages 853-863, ISSN 0223-5234, https://doi.org/10.1016/j.ejmech.2018.12.0220223-5234http://hdl.handle.net/2183/40681This is an accepted version of the published document.[Abstract] Two new ruthenium complexes, [Ru(η5-Cp)(PPh3)(2,2’-bipy-4,4’-R)]+ with R = -CH2OH (Ru1) or dibiotin ester (Ru2) were synthesized and fully characterized. Both compounds were tested against two types of breast cancer cells (MCF7 and MDA-MB-231), showing better cytotoxicity than cisplatin in the same experimental conditions. Since multidrug resistance (MDR) is one of the main problems in cancer chemotherapy, we have assessed the potential of these compounds to overcome resistance to treatments. Ru2 showed exceptional selectivity as P-gp inhibitor, while Ru1 is possibly a substrate. In vivo studies in zebrafish showed that Ru2 is well tolerated up to 1.17 mg/L, presenting a LC50 of 5.73 mg/L at 5 days post fertilization.engAtribución-NoComercial-SinDerivadas 4.0 Internacionalhttp://creativecommons.org/licenses/by-nc-nd/4.0/Ruthenium organometallic compoundsAnticancer agentsP-gp inhibitorMultidrug resistancejournal articleopen access10.1016/j.ejmech.2018.12.022