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G‐Quadruplex Recognition by Quinacridines: a SAR, NMR, and Biological Study
Author(s) -
Hounsou Candide,
Guittat Lionel,
Monchaud David,
Jourdan Muriel,
Saettel Nicolas,
Mergny JeanLouis,
TeuladeFichou MariePaule
Publication year - 2007
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200600286
Subject(s) - g quadruplex , chemistry , dna , computational biology , combinatorial chemistry , förster resonance energy transfer , biochemistry , biology , fluorescence , physics , quantum mechanics
The synthesis of a novel group of quinacridine‐based ligands (MMQs) is described along with an evaluation of their G‐quadruplex binding properties. A set of biophysical assays was applied to characterize their interaction with DNA quadruplexes: FRET–melting experiments and equilibrium microdialysis were used to evaluate their quadruplex affinity and their ability to discriminate quadruplexes across a broad panel of DNA structures. All data collected support the proposed model of interaction of these compounds with G‐quadruplexes, which is furthermore confirmed by a solution structure determined by 2D NMR experiments. Finally, the activity of the MMQ series against tumor cell growth is reported, and the data support the potential of quadruplex‐interactive compounds for use in anticancer approaches.