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- Methyl-cyclopentadienyl ruthenium compounds with 2,2 '-bipyridine derivatives display strong anticancer activity and multidrug resistance potentialPublication . Côrte-Real, Leonor; Gonçalves Teixeira, Ricardo; Girio, Patrícia; Comsa, Elisabeta; MORENO, Alexis; Nasr, Rachad; Baubichon-Cortay, Helene; Avecilla, Fernando; Marques, Fernanda; Robalo, Maria Paula; Mendes, Paulo; Prates Ramalho, João P.; Garcia; Falson, Pierre; Valente, AndreiaNew ruthenium methyl-cyclopentadienyl compounds bearing bipyridine derivatives with the general formula [Ru(eta(5)-MeCp)(PPh3)(4,4'-R-2,2'-bpy)](+) (Ru1, R = H; Ru2, R = CH3; and Ru3, R = CH2OH) have been synthesized and characterized by spectroscopic and analytical techniques. Ru1 crystallized in the monoclinic P2(1)/c, Ru2 in the triclinic P (1) over bar, and Ru3 in the monoclinic P2(1)/n space group. In all molecular structures, the ruthenium center adopts a "piano stool" distribution. Density functional theory calculations were performed for all complexes, and the results support spectroscopic data. Ru1 and Ru3 were poor substrates of the main multidrug resistance human pumps, ABCB1, ABCG2, ABCC1, and ABCC2, while Ru2 displayed inhibitory properties of ABCC1 and ABCC2 pumps. Importantly, all compounds displayed a very high cytotoxic profile for ovarian cancer cells (sensitive and resistant) that was much more pronounced than that observed with cisplatin, making them very promising anticancer agents.
- Novel ruthenium methylcyclopentadienyl complex bearing a bipyridine perfluorinated ligand shows strong activity towards colorectal cancer cellsPublication . Gonçalves Teixeira, Ricardo; Brás, Ana Rita; Côrte-Real, Leonor; Tatikonda, Rajendhraprasad; Sanches, Anabela; Robalo, Maria Paula; Avecilla, Fernando; Moreira, Tiago; Garcia, M. Helena; Haukka, Matti; Preto, Ana; Valente, AndreiaThree new compounds have been synthesized and completely characterized by analytical and spectroscopic techniques. The new bipyridine-perfluorinated ligand L1 and the new organometallic complex [Ru(η5-MeCp)(PPh3)2Cl] (Ru1) crystalize in the centrosymmetric triclinic space group P
1¯. Analysis of the phenotypic effects induced by both organometallic complexes Ru1 and [Ru(η5-MeCp)(PPh3)(L1)][CF3SO3] (Ru2), on human colorectal cancer cells (SW480 and RKO) survival, showed that Ru2 has a potent anti-proliferative activity, 4–6 times higher than cisplatin, and induce apoptosis in these cells. Data obtained in a noncancerous cell line derived from normal colon epithelial cells (NCM460) revealed an intrinsic selectivity of Ru2 for malignant cells at low concentrations, showing the high potential of this compound as a selective anticancer agent.