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Ruthenium-based PACT agents based on bisquinoline chelates: synthesis, photochemistry, and cytotoxicity by Anja Busemann; Ingrid Flaspohler; Xue-Quan Zhou; Claudia Schmidt; Sina K. Goetzfried; Vincent H. S. van Rixel; Ingo Ott; Maxime A. Siegler; Sylvestre Bonnet is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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## Abstract The known ruthenium complex [Ru(tpy)(bpy)(Hmte)](PF~6~)~2~ ([1](PF~6~)~2~, where tpy = 2,2’:6’,2′′-terpyridine, bpy = 2,2’-bipyridine, Hmte = 2-(methylthio)ethanol) is photosubstitutionally active but non-toxic to cancer cells even upon light irradiation. In this work, the two analogs complexes [Ru(tpy)(NN)(Hmte)](PF~6~)~2~, where NN = 3,3'-biisoquinoline (i-biq, [2](PF~6~)~2~) and di(isoquinolin-3-yl)amine (i-Hdiqa, [3](PF~6~)~2~), were synthesized and their photochemistry and phototoxicity evaluated to assess their suitability as photoactivated chemotherapy (PACT) agents. The increase of the aromatic surface of [2](PF~6~)~2~ and [3](PF~6~)~2~, compared to [1](PF~6~)~2~, leads to higher lipophilicity and higher cellular uptake for the former complexes. Such improved uptake is directly correlated to the cytotoxicity of these compounds in the dark: while [2](PF~6~)~2~ and [3](PF~6~)~2~ showed low EC~50~ values in human cancer cells, [1](PF~6~)~2~ is not cytotoxic due to poor cellular uptake. While stable in the dark, all complexes substituted the protecting thioether ligand upon light irradiation (520 nm), with the highest photosubstitution quantum yield found for [3](PF

Who reads Ruthenium-based PACT agents based on bisquinoline chelates: synthesis, photochemistry, and cytotoxicity?

Author

Anja Busemann; Ingrid Flaspohler; Xue-Quan Zhou; Claudia Schmidt; Sina K. Goetzfried; Vincent H. S. van Rixel; Ingo Ott; Maxime A. Siegler; Sylvestre Bonnet

Publisher

Springer Science and Business Media LLC

Published

2021

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)