Abstract

Strained ruthenium (Ru) complexes have been synthesized and characterized as novel agents for photodynamic therapy (PDT). The complexes are inert until triggered by visible light, which induces ligand loss and covalent modification of DNA. An increase in cytotoxicity of 2 orders of magnitude is observed with light activation in cancer cells, and the compounds display potencies superior to cisplatin against 3D tumor spheroids. The use of intramolecular strain may be applied as a general paradigm to develop light-activated ruthenium complexes for PDT applications.

Keywords

RutheniumChemistryIntramolecular forceCytotoxicityCovalent bondCisplatinLigand (biochemistry)Photodynamic therapyPhotochemistryCombinatorial chemistryBiophysicsStereochemistryIn vitroBiochemistryCatalysisOrganic chemistryReceptorChemotherapy

MeSH Terms

Antineoplastic AgentsCell LineTumorCell SurvivalCoordination ComplexesDNAHumansLightNeoplasmsPhotochemotherapyPhotosensitizing AgentsRuthenium

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Publication Info

Year
2012
Type
article
Volume
134
Issue
20
Pages
8324-8327
Citations
485
Access
Closed

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485
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3
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470
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Cite This

Brock S. Howerton, David K. Heidary, Edith C. Glazer (2012). Strained Ruthenium Complexes Are Potent Light-Activated Anticancer Agents. Journal of the American Chemical Society , 134 (20) , 8324-8327. https://doi.org/10.1021/ja3009677

Identifiers

DOI
10.1021/ja3009677
PMID
22553960

Data Quality

Data completeness: 81%