Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 23, Issue 35, Pages 8491-8499Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201700957
Keywords
circular dichroism; DNA; G-quadruplex; naphthalenediimide; structure-activity relationships
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Funding
- British Council-DST UKIERI
- University of Bath
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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 (N-epsilon-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.
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