Abstract
KGaA, Weinheim. 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(ɤNN)(C≡NtBu)]ClO4(1 a, HɤNN= 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.
Original language | English |
---|---|
Pages (from-to) | 10120-10123 |
Number of pages | 4 |
Journal | Angewandte Chemie - International Edition |
Volume | 53 |
Issue number | 38 |
DOIs | |
Publication status | Published - 15 Sep 2014 |
Keywords
- anticancer
- DNA
- exciplex emission
- platinum
- topoisomerase I
ASJC Scopus subject areas
- Catalysis
- Chemistry(all)