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- Title
Mitochondrial‐DNA‐Targeted Ir<sup>III</sup>‐Containing Metallohelices with Tunable Photodynamic Therapy Efficacy in Cancer Cells.
- Authors
Li, Xuezhao; Wu, Jinguo; Wang, Lei; He, Cheng; Chen, Liyong; Jiao, Yang; Duan, Chunying
- Abstract
The development of DNA‐targeted photodynamic therapy (PDT) agents for cancer treatment has drawn substantial attention. Herein, the design and synthesis of dinuclear IrIII‐containing luminescent metallohelices with tunable PDT efficacy that target mitochondrial DNA in cancer cells are reported. The metallohelices are fabricated using dynamic imine‐coupling chemistry between aldehyde end‐capped fac‐Ir(ppy)3 handles and linear alkanediamine spacers, followed by reduction of the imine linkages. The length and odd–even character of the diamine alkyl linker determined the stereochemistry (helicates vs. mesocates). Compared to the helicates, the mesocates exhibit improved apoptosis‐induction upon white‐light irradiation. Molecular docking studies indicate that the mesocate with a proper length of diamine spacers shows stronger affinity for the minor groove of DNA. This study highlights the potential of DNA‐targeting IrIII‐containing metallohelices as PDT agents.
- Subjects
PHOTODYNAMIC therapy; CANCER cells; CANCER treatment; MOLECULAR docking; STEREOCHEMISTRY; MITOCHONDRIAL DNA
- Publication
Angewandte Chemie, 2020, Vol 132, Issue 16, p6482
- ISSN
0044-8249
- Publication type
Article
- DOI
10.1002/ange.201915281