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Methylene-linked bis-phenylbenzimidazoles – a new scaffold to target telomeric DNA/RNA hybrid duplex

Research output: Contribution to journalArticle

Original languageEnglish
Pages (from-to)4424–4428
Number of pages5
JournalORGANIC AND BIOMOLECULAR CHEMISTRY
Volume16
Issue number24
Early online date2 Mar 2018
DOIs
Accepted/In press12 Jan 2018
E-pub ahead of print2 Mar 2018
Published2018

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Abstract

We report a series of novel methylene-linked bis-phenylbenzimidazoles intercalators that stabilize telomeric DNA/RNA hybrid (tDRH) structures by up to 7.2 °C at a 1 μM ligand concentration while having negligible affinity for DNA/DNA duplexes, although with a low affinity for quadruplex DNA. We have used molecular modelling studies to rationalize this selectivity, concluding that the methylene spacer between the terminal benzimidazole and phenylene moieties plays a key role in facilitating the bis-intercalating process. This scaffold may be used to develop chemical tools or new therapeutics to selectively target the telomeric DNA/RNA duplex without affecting normal genomic DNA.

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