Abstract
A series of platinum(II) complexes containing dipyridophenazine (dppz) and C-deprotonated 2-phenylpyridine (N∧CH) ligands were prepared and assayed for G-quadruplex DNA binding activities. [PtII(dppz-COOH)(N∧C)]CF3SO3 (1; dppz-COOH = 11-carboxydipyrido[3,2-a:2′,3′-c]phenazine) binds G-quadruplex DNA through an external end-stacking mode with a binding affinity of ∼107 dm3 mol−1. G-quadruplex DNA binding is accompanied by up to a 293-fold increase in the intensity of photoluminescence at λmax = 512 nm. Using a biotinylated-primer extension telomerase assay, 1 was shown to be an effective inhibitor of human telomerase in vitro, with a telIC50 value of 760 nM.
Original language | English |
---|---|
Pages (from-to) | 1835-1846 |
Number of pages | 12 |
Journal | Journal of the American Chemical Society |
Volume | 131 |
Issue number | 5 |
DOIs | |
Publication status | Published - 11 Feb 2009 |
Scopus Subject Areas
- Catalysis
- General Chemistry
- Biochemistry
- Colloid and Surface Chemistry
User-Defined Keywords
- Biopolymers
- G-Quadruplex
- Genetics
- Ligands
- Peptides and proteins