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

Dora-Maria Rasadean, Bin Sheng, Jyotirmayee Dash, G. Dan Pantos

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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 (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.

Original languageEnglish
Pages (from-to)8491-8499
Number of pages9
JournalChemistry - A European Journal
Issue number35
Early online date24 May 2017
Publication statusPublished - 23 Jun 2017


  • circular dichroism
  • DNA
  • G-quadruplex
  • naphthalenediimide
  • structure–activity relationships

ASJC Scopus subject areas

  • Chemistry(all)


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