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The popularity of RAPTA-C in in vivo studies has steered the way for complexes of the type [Ru(η⁶-arene)(X)(Y)(Z)]ⁿ⁺ (where X, Y and Z are monodentate ligands) to be developed for biological, primarily, anticancer applications. This has led them to become a class of their own, with extensive research in this area happening over the past decade. The choice of three monodentate ligands plus the arene in the piano-stool skeleton of these complexes allows the researchers to control and tweak their chemical properties dexterously. These complexes are tuned to inhibit various enzyme functions or selectively target specific cancer cell lines by integrating appropriate ligands into the system. Ligands with biological relevance synergistically enhance the overall activity, which has been the key basis for constructing such complex systems. The activation mechanism of these bifunctional complexes involves the hydrolysis …