Street, Steven T. G. , Chin, Donovan, Hollingworth, Greg, Berry, Monica, Morales, Juan C. and Galan, M. Carmen (2017) Divalent Naphthalene Diimide Ligands Display High Selectivity for the Human Telomeric G-quadruplex in K+ buffer. Chemistry - a European journal, 23 (29). pp. 6953-6958. ISSN 09476539

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.

Item Type:	Article
Date Deposited:	01 Jul 2017 00:45
Last Modified:	01 Jul 2017 00:45
URI:	https://oak.novartis.com/id/eprint/31020