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J Med Chem. 2017 Nov 9;60(21):8923-8932. doi: 10.1021/acs.jmedchem.7b01162. Epub 2017 Oct 19.

A Smart Europium-Ruthenium Complex as Anticancer Prodrug: Controllable Drug Release and Real-Time Monitoring under Different Light Excitations.

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Department of Chemistry, Hong Kong Baptist University , Kowloon Tong, Hong Kong SAR.
Department of Cell Biology and Medical Genetics, School of Medicine, Shenzhen University , Shenzhen, Guangdong, China.
Department of Applied Biological and Chemical Technology, The Hong Kong Polytechnic University , Hung Hum, Hong Kong SAR.
School of Chemistry and Environment Engineering, Hanshan Normal University , Chaozhou 521041, Guangdong, China.
Institute of Chemical Sciences & Engineering, Swiss Federal Institute of Technology, Lausanne (EPFL) , CH-1015 Lausanne, Switzerland.


A unique, dual-function, photoactivatable anticancer prodrug, RuEuL, has been tailored that features a ruthenium(II) complex linked to a cyclen-europium chelate via a π-conjugated bridge. Under irradiation at 488 nm, the dark-inactive prodrug undergoes photodissociation, releasing the DNA-damaging ruthenium species. Under evaluation-window irradiation (λirr = one-photon 350 nm or two-photon 700 nm), the drug delivery process can be quantitatively monitored in real-time because of the long-lived red europium emission. Linear relationships between released drug concentration and ESI-MS or luminescence responses are established. Finally, the efficiency of the new prodrug is demonstrated both in vitro RuEuL anticancer prodrug over some existing ones and open the way for decisive improvements in multipurpose prodrugs.

[Indexed for MEDLINE]

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