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DNA-Targeting RuII-Polypyridyl Complex with a Long-Lived Intraligand Excited State as a Potential Photodynamic Therapy Agent
Authors:Wuyang Hua  Dr Gang Xu  Dr Jian Zhao  Dr Z Wang  Jiapeng Lu  Prof Wenfang Sun  Prof Shaohua Gou
Institution:1. Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research and Pharmaceutical Research Center, School of Chemistry and Chemical, Engineering, Southeast University, Nanjing, 211189 P.R. China

These authors contributed equally to this work.;2. Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research and Pharmaceutical Research Center, School of Chemistry and Chemical, Engineering, Southeast University, Nanjing, 211189 P.R. China;3. Department of Chemistry and Biochemistry, North Dakota State University, Fargo, North Dakota, 58108-6050 USA

Abstract:Subtle ligand modifications on RuII-polypyridyl complexes may result in different excited-state characteristics, which provides the opportunity to tune their photo-physicochemical properties and subsequently change their biological functions. Here, a DNA-targeting RuII-polypyridyl complex (named Ru1 ) with highly photosensitizing 3IL (intraligand) excited state was designed based on a classical DNA-intercalator Ru(bpy)2(dppz)] ⋅ 2 PF6 by incorporation of the dppz (dipyrido3,2-a:2′,3′-c]phenazine) ligand tethered with a pyrenyl group, which has four orders of magnitude higher potency than the model complex Ru(bpy)2(dppz)] ⋅ 2 PF6 upon light irradiation. This study provides a facile strategy for the design of organelle-targeting RuII-polypyridyl complexes with dramatically improved photobiological activity.
Keywords:DNA  photodynamics  reactive oxygen species (ROS)  Ru polypyridyl complexes
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