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- Title
Divalent Naphthalene Diimide Ligands Display High Selectivity for the Human Telomeric G-quadruplex in K<sup>+</sup> Buffer.
- Authors
Street, Steven T. G.; Chin, Donovan N.; Hollingworth, Gregory J.; Berry, Monica; Morales, Juan C.; Galan, M. Carmen
- Abstract
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 herein. 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.
- Subjects
NAPHTHYL compounds; IMIDES; LIGAND exchange reactions; COORDINATION compounds; LIGANDS (Chemistry)
- Publication
Chemistry - A European Journal, 2017, Vol 23, Issue 29, p6953
- ISSN
0947-6539
- Publication type
Article
- DOI
10.1002/chem.201700140