Luminescent Cyclometalated Platinum(II) Complex Forms Emissive Intercalating Adducts with Double‐Stranded DNA and RNA: Differential Emissions and Anticancer Activities |
| |
| Authors: | Taotao Zou Dr Jia Liu Dr Ching Tung Lum Dr Chensheng Ma Ruth Chau‐Ting Chan Dr Chun‐Nam Lok Dr Wai‐Ming Kwok Prof?Dr Chi‐Ming Che |
| |
| Institution: | 1. State Key Laboratory of Synthetic Chemistry, Institute of Molecular Functional Materials, Chemical Biology Centre and Department of Chemistry, The University of Hong Kong, Pokfulam Road, Hong Kong (China);2. Current address: School of Chemistry and Chemical Engineering, Shenzhen University (China);3. Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong (China);4. HKU Shenzhen Institute of Research and Innovation, Shenzhen 518053 (China) |
| |
| Abstract: | Luminescent metallo‐intercalators are potent biosensors of nucleic acid structure and anticancer agents targeting DNAs. There are few examples of luminescent metallo‐intercalators which can simultaneously act as emission probes of nucleic acid structure and display promising anticancer activities. Herein, we describe a luminescent platinum(II) complex, Pt(C^N^N)(C≡NtBu)]ClO4 ( 1 a , HC^N^N= 6‐phenyl‐2,2′‐bipyridyl), that intercalates between the nucleobases of nucleic acids, accompanied by an increase in emission intensity and/or a significant change in the maximum emission wavelength. The changes in emission properties measured with double‐stranded RNA (dsRNA) are different from those with dsDNA used in the binding reactions. Complex 1 a exhibited potent anticancer activity towards cancer cells in vitro and inhibited tumor growth in a mouse model. The stabilization of the topoisomerase I–DNA complex with resulting DNA damage by 1 a is suggested to contribute to its anticancer activity. |
| |
| Keywords: | anticancer DNA exciplex emission platinum topoisomerase I |
|
|
