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

AutorStreet, Steven T. G.; Chin, Donovan N.; Hollingworth, Gregory J.; Berry, Monica; Morales, Juan C.; Galan, M. Carmen
Palabras claveAntitumour agents
Carbohydrates
Drug design
G-quadruplexes
Molecular recognition
Fecha de publicación30-mar-2017
EditorJohn Wiley & Sons
CitaciónChemistry - a European Journal
ResumenSelective 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.
Versión del editorhttps://onlinelibrary.wiley.com/doi/abs/10.1002/chem.201700140
URIhttp://hdl.handle.net/10261/163349
DOI10.1002/chem.201700140
ISSN0947-6539
E-ISSN1521-3765
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