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Issue 24, 2018
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Methylene-linked bis-phenylbenzimidazoles – a new scaffold to target telomeric DNA/RNA hybrid duplex

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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.

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

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Supplementary files

Article information


Submitted
03 Nov 2017
Accepted
12 Jan 2018
First published
02 Mar 2018

Org. Biomol. Chem., 2018,16, 4424-4428
Article type
Communication

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

M. K. Islam, P. J. M. Jackson, D. E. Thurston and K. M. Rahman, Org. Biomol. Chem., 2018, 16, 4424
DOI: 10.1039/C7OB02709E

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