期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 60, 期 21, 页码 8923-8932出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b01162
关键词
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资金
- Hong Kong Research Grants Council [HKBU 12309516]
- HKBU [FRG 2/16-17/016]
- National Natural Science Foundation of China [21402167, 21401035]
- Natural Science Foundation of Guangdong Province [2014A030307027]
- Dr Kennedy Y. H. Wong Distinguished Visiting Professorship Scheme, Hong Kong Baptist University
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 pi-conjugated bridge. Under irradiation at 488 nm, the dark-inactive prodrug undergoes photodissociation, releasing the DNA-damaging ruthenium species. Under evaluation window irradiation (lambda(irr) = 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.
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