Publication Type Journal Article
Title Unprecedented inhibition of P-gp activity by a novel ruthenium-cyclopentadienyl compound bearing a bipyridine-biotin ligand
Authors Leonor Côrte-Real Brittany Karas Patricia Girio Alexis Moreno Fernando Avecilla Fernanda M. Marques Brian T. Buckley Keith R. Cooper Cathleen Doherty Pierre Falson M. Helena Garcia Andreia Valente
Groups BIOIN
Journal EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Year 2019
Month February
Volume 163
Number
Pages 853-863
Abstract Two new ruthenium complexes, [Ru(eta(5)-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. (C) 2018 Elsevier Masson SAS. All rights reserved.
DOI http://dx.doi.org/10.1016/j.ejmech.2018.12.022
ISBN
Publisher
Book Title
ISSN 0223-5234
EISSN 1768-3254
Conference Name
Bibtex ID ISI:000458597300062
Observations
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