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  • Title: Benzo(h)quinoline derivatives as G-quadruplex binding agents.
    Author: Paritala H, Firestine SM.
    Journal: Bioorg Med Chem Lett; 2009 Mar 15; 19(6):1584-7. PubMed ID: 19243943.
    Abstract:
    G-quadruplexes are unusual structures formed from guanine-rich sequences of nucleic acids. G-quadruplexes have been postulated to play important roles in a number of biological systems including gene regulation and the inhibition of enzyme function. Recently, our laboratory reported on the synthesis and evaluation of a triaza-cyclopentaphenanthrene compound which bound to G-quadruplexes with good affinity and selectivity. This compound contains a 4-pyridone group which has not been previously utilized in other quadruplex binding agents. In this Letter, we describe the synthesis and evaluation of 4-pyridone containing 2- and 3-carboxy-benzoquinolines as G-quadruplex binding agents. We find that these compounds are capable of binding G-quadruplexes with a K(a) in the range of 3 x 10(5)M(-1) and with a 10-fold selectivity for quadruplex over duplex DNA.
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