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Issue 7, 2004
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Synthesis and evaluation of analogues of 10H-indolo[3,2-b]quinoline as G-quadruplex stabilising ligands and potential inhibitors of the enzyme telomerase

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Abstract

We report here the synthesis and evaluation for telomerase-inhibitory and quadruplex DNA binding properties of several rationally-designed quindoline analogues, substituted at the 2- and 7- positions. The ability of these compounds to interact with and stabilise an intramolecular G-quadruplex DNA against increases in temperature was evaluated by a fluorescence-based (FRET) melting assay. The resulting Tm values were found to correlate with their potency for telomerase inhibition, as measured in an in vitro telomerase TRAP assay. The interactions of a number of compounds with a quadruplex DNA molecular structure were simulated by molecular modelling methods. It is concluded that this class of compound represents a new chemical type suitable for further development as telomerase inhibitors.

Graphical abstract: Synthesis and evaluation of analogues of 10H-indolo[3,2-b]quinoline as G-quadruplex stabilising ligands and potential inhibitors of the enzyme telomerase

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Publication details

The article was received on 08 Dec 2003, accepted on 18 Feb 2004 and first published on 10 Mar 2004


Article type: Paper
DOI: 10.1039/B316055F
Org. Biomol. Chem., 2004,2, 981-988

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    Synthesis and evaluation of analogues of 10H-indolo[3,2-b]quinoline as G-quadruplex stabilising ligands and potential inhibitors of the enzyme telomerase

    B. Guyen, C. M. Schultes, P. Hazel, J. Mann and S. Neidle, Org. Biomol. Chem., 2004, 2, 981
    DOI: 10.1039/B316055F

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