Divalent Naphthalene Diimide Ligands Display High Selectivity for the Human Telomeric G-quadruplex in K+ Buffer

Steve Street, Donovan N. Chin, Gregory J Hollingworth, Monica Berry, Juan Carlos Morales, Carmen Galan

Research output: Contribution to journalArticle (Academic Journal)peer-review

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Selective G-quadruplex ligands offer great promise for the development of anti-cancer therapies. A novel series of divalent cationic naphthalene diimide ligands that selectively bind to the hybrid form of the human telomeric G-quadruplex in K+ buffer are described here. We demonstrate that an imidazolium-bearing mannoside-conjugate is the most selective ligand to date for this quadruplex against several other quadruplex and duplex structures. We also show that a similarly selective methylpiperazine-bearing ligand was more toxic to HeLa cancer cells than doxorubicin, whilst exhibiting three times less toxicity towards fetal lung fibroblasts WI-38.
Original languageEnglish
Pages (from-to)6953-6958
Number of pages6
JournalChemistry - A European Journal
Issue number29
Early online date30 Mar 2017
Publication statusPublished - 3 May 2017

Structured keywords

  • BCS and TECS CDTs


  • Antitumour agents
  • Carbohydrates
  • Drug design
  • G-quadrupexes
  • Molecular recognition

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