Development of Organometallic Ruthenium-Arene Anticancer Drugs That Resist Hydrolysis

With a view to develop drugs that could resist hydrolysis in aq. media,organometallic arene-capped ruthenium(II) 1,3,5-triaza-7-phosphatricyclo[3.3.1.1]decane (RAPTA) complexes bearing chelating carboxylate ligands have been prepd. and studied. The new complexes, Ru(η6-cymene)(PTA)(C2O4) (1) and Ru(η6-cymene)(PTA)(C6H6O4) (2), were found to be highly sol. and kinetically more stable than their RAPTA precursor that contains two chloride ligands in place of the carboxylate ligands. They were also able to resist hydrolysis in water and exhibited significantly lower pKa values. Importantly, they showed a similar order of activity in inhibiting cancer cell-growth proliferation (as detd. by in vitro assays) and exhibited oligonucleotide binding characteristics (as evidenced by matrix-assisted laser desorption ionization mass spectrometry) similar to those of the RAPTA precursor, hence realizing a strategy for developing a new generation of stable and highly water-sol. RAPTA adducts.

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Paul Joseph Dyson, Wee Han Ang, Claudine Scolaro, Elisa Daldini
2006
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https://infoscience.epfl.ch/record/90798?ln=en

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Bridging ligand

In coordination chemistry, a bridging ligand is a ligand that connects two or more atoms, usually metal ions. The ligand may be atomic or polyatomic. Virtually all complex organic compounds can serve as bridging ligands, so the term is usually restricted to small ligands such as pseudohalides or to ligands that are specifically designed to link two metals. In naming a complex wherein a single atom bridges two metals, the bridging ligand is preceded by the Greek letter mu, μ, with a subscript number denoting the number of metals bound to the bridging ligand.

Ligand

In coordination chemistry, a ligand is an ion or molecule with a functional group that binds to a central metal atom to form a coordination complex. The bonding with the metal generally involves formal donation of one or more of the ligand's electron pairs, often through Lewis bases. The nature of metal–ligand bonding can range from covalent to ionic. Furthermore, the metal–ligand bond order can range from one to three. Ligands are viewed as Lewis bases, although rare cases are known to involve Lewis acidic "ligands".

Tridentate ligand

A tridentate ligand (or terdentate ligand) is a ligand that has three atoms that can function as donor atoms in a coordination complex. Well-known tridentate ligands include diethylenetriamine with three nitrogen donor atoms, and the iminodiacetate anion which consists of one deprotonated amine nitrogen and a pair of carboxylate groups. An octahedrally coordinated atom has six positions around it. Two tridentate ligands may form a complex with such an atom.