3 years ago

Amino-Acid-Derived Naphthalenediimides as Versatile G-Quadruplex Binders

Amino-Acid-Derived Naphthalenediimides as Versatile G-Quadruplex Binders
Dora M. Răsădean, G. Dan Pantoş, Jyotirmayee Dash, Bin Sheng
The design and synthesis of water soluble, amino-acid-functionalised naphthalenediimides (NDIs) as potential ligands of native G-quadruplexes is reported. The NDIs were tested on a panel of oncogene promoters, on the human telomeric sequence h-telo, and on double-stranded DNA. Out of the ligands tested, NDI 3 (Nϵ-Boc-l-lysine NDI) exhibited a highly discriminating nature by only stabilising the oncogene promoter c-kit2, which is up-regulated up to 80 % in ovarian, gastrointestinal, and breast malignancies. Selective oncogene stablilisation: Water-soluble, amino acid functionalised naphthalenediimides are potential ligands of native G-quadruplexes, and they are tested on a panel of oncogene promoters and against double-strand DNA. One of the ligands, NDI 3, exhibits a highly discriminating nature by stabilising only the oncogene promoter c-kit2, which is upregulated up to 80 % in ovarian, gastrointestinal, and breast malignancies (see figure).

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/chem.201700957

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