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Abstract: The design of more efficient anticancer drugs requires a deeper understanding of their biodistribution and mechanism of action. Cell imaging agents could help to gain insight into biological processes and, consequently, the best strategy for attaining suitable scaffolds in which both biological and imaging properties are maximized. A new concept arises in this field that is the combination of two metal fragments as collaborative partners to provide the precise emissive properties to visualize the cell as well as the optimum cytotoxic activity to build more potent and selective chemotherapeutic agents. [ABSTRACT FROM AUTHOR]

Abstract: A mutifunctional ruthenium‐based conjugate Ru‐BSe was designed and synthesized. The Ru complex with favorable bioimaging function was covalently linked with a cancer‐targeted molecule that could be effectively internalized by the tumor to realize enhanced theranostic effects. The pH‐response of the Ru conjugate in tumor acidic microenvironment causes ligand substitution and release of therapeutic complex. This activated complex remains inert to the reducing biomolecule‐glutathione and terminally locates in mitochondria, in which it triggers oxidative stress, and activates intrinsic apoptosis. Real‐time monitoring reveals that this Ru conjugate could selectively accumulate in tumor tissue in vivo, which significantly suppresses tumor progression and alleviate the damage to normal organs, realizing the precise cancer theranosis. [ABSTRACT FROM AUTHOR]