Red-Light Activation of a Microtubule Polymerization Inhibitor via Amide Functionalization of the Ruthenium Photocage

Published in: Angew Chem Int Ed

Authors: Ludovic Bretin, Yurii Husiev, Vadde Ramu, Liyan Zhang, Matthijs Hakkennes, Selda Abyar, Andrew C. Johns, Sylvia E. Le Dévédec, Tania Betancourt, Alexander Kornienko, Sylvestre Bonnet

Leiden University

A ruthenium-based compound was developed for PACT (photoactivated chemotherapy), which unlike most existing PACT compounds, can be also activated with clinically relevant longer (red) wavelength of light. ML6600 was used for in vivo experiments to superficially activate PACT compound in subcutaneous tumor comparing green and red wavelengths. The tumor volume reduction was significant (45%) upon red light irradiation compared with vehicle control, and statistically identical with that obtained upon green light activation. Also biosafety of the compound was improved, leading to lower toxicity of the prodrug in the dark, both in vitro and in vivo.


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