Department of Chemistry, University of Kentucky, Lexington, 40506, United States.
J Am Chem Soc. 2012 May 23;134(20):8324-7. doi: 10.1021/ja3009677. Epub 2012 May 11.
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.
已合成并表征了应变钌（Ru）配合物，将其作为光动力疗法（PDT）的新型试剂。这些配合物在可见光触发之前是惰性的，可见光触发会导致配体丢失和 DNA 的共价修饰。在癌细胞中用光激活时，观察到细胞毒性增加了 2 个数量级，并且这些化合物对 3D 肿瘤球体的效力优于顺铂。可以将使用分子内应变作为一般范例来开发用于 PDT 应用的光激活钌配合物。
