Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 10, Issue 14, Pages 2798-2806Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2ob06816h
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Funding
- MIUR [FIRB-Ideas RBID082ATK]
- Associazione Italiana per la Ricerca sul Cancro [AIRC 5826 and 8861]
- Pavia University
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The synthesis, physico-chemical properties and biological effects of a new class of naphthalene diimides (NDIs) capable of reversibly binding telomeric DNA and alkylate it through an electrophilic quinone methide moiety (QM), are reported. FRET and circular dichroism assays showed a marked stabilization and selectivity towards telomeric G4 DNA folded in a hybrid topology. NDI-QMs' alkylating properties revealed a good reactivity on single nucleosides and selectivity towards telomeric G4. A selected NDI was able to significantly impair the growth of melanoma cells by causing telomere dysfunction and down-regulation of telomerase expression. These findings points to our hybrid ligand-alkylating NDIs as possible tools for the development of novel targeted anticancer therapies.
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