Publication 15 of year 2022

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  1. Optochemical Control of Therapeutic Agents through Photocatalyzed Isomerization
    Winssinger, N.; Watson, E. E.; Russo, F.; Moreau, D.
    Angew. Chem. Int. Ed., in press

 

A Ru(bpy) 3 photocatalyst is applied to the rapid trans to cis isomerization of a range of alkene-containing pharmacological agents, including combretastatin (CA-4), a clinical candidate in oncology, and resveratrol derivatives, switching their configuration from inactive substances to potent cytotoxic agents. Selective in cellulo activation of the CA-4 analog Res-3M is demonstrated, along with its potent cytotoxicity and inhibition of microtubule dynamics.

DOI: 10.1002/anie.202203390