- DMSO-mediated ligand dissociation: Renaissance for biological activity of N-heterocyclic-[Ru(η6-arene)Cl2] drug candidates
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Slipped under the radar? 1HNMR spectroscopic examination revealed that [Ru(η6-arene)Cl2(L)] (L=N-heterocyclic ligands) complexes readily undergo a ligand exchange reaction in DMSO (see scheme), a popular medium for preparing stock solutions for biological screening. It is therefore highly important for researchers to study the stability in DMSO before reporting on the biological activity of such complexes. Copyright
- Patra, Malay,Joshi, Tanmaya,Pierroz, Vanessa,Ingram, Katrin,Kaiser, Marcel,Ferrari, Stefano,Spingler, Bernhard,Keiser, Jennifer,Gasser, Gilles
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- Conjugating Biotin to Ruthenium(II) Arene Units via Phosphine Ligand Functionalization
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Two-step functionalization of 4-diphenylphosphino benzoic acid with biotin afforded 2-(biotinyloxy)ethyl 4-(diphenylphosphanyl)benzoate (LP), that was subsequently used to synthesize the Ru(II) arene complexes [RuCl2(η6-p-cymene)(LP)] (1), [Ru(C2O4)(η6-p-cymene)(LP)] (2) and [Ru(curc)(η6-p-cymene)(LP)]NO3 ([3]NO3), the latter incorporating curcumin (curcH) as an additional bioactive fragment. [Ru(curc)(η6-p-cymene)(PPh3)]NO3 ([4]NO3) was also prepared as a reference compound. Compounds 2 and [3]NO3 exhibited excellent stability in water/DMSO solution while being slowly activated in the cell culture medium over 72 hours. Together with LP, they were therefore assessed for their antiproliferative activity towards a panel of cancer cell lines, with different levels of biotin transporter expression. The apparent affinity of the compounds towards avidin varies, and their antiproliferative activity does not correlate with biotin transporter expression, although it is systematically enhanced when biotin-free cell culture medium is used.
- B?au?, Andrzej,Batchelor, Lucinda K.,Biancalana, Lorenzo,Dyson, Paul J.,Grucha?a, Martyna,Marchetti, Fabio,Monti, Andrea,Pampaloni, Guido,Rychlik, B?a?ej
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