Macrocyclic Pyridyl Polyoxazoles: Selective RNA and DNA G-Quadruplex Ligands as Antitumor Agents
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چکیده
منابع مشابه
Macrocyclic Pyridyl Polyoxazoles: Structure-Activity Studies of the Aminoalkyl Side-Chain on G-Quadruplex Stabilization and Cytotoxic Activity
Pyridyl polyoxazoles are 24-membered macrocyclic lactams comprised of a pyridine, four oxazoles and a phenyl ring. A derivative having a 2-(dimethylamino)ethyl chain attached to the 5-position of the phenyl ring was recently identified as a selective G-quadruplex stabilizer with excellent cytotoxic activity, and good in vivo anticancer activity against a human breast cancer xenograft in mice. H...
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Ligands Pravin S. Shirude,† Elizabeth R. Gillies,‡ Sylvain Ladame,† Frédéric Godde,‡ Kazuo Shin-ya,§ Ivan Huc,*,‡ and Shankar Balasubramanian*,† UniVersity Chemical Laboratory, UniVersity of Cambridge, Lensfield Road, Cambridge CB2 1EW, U.K., Institut Européen de Chimie et Biologie, UniVersité Bordeaux 1-CNRS UMR 5248, 2 rue Robert Escarpit, 33607 Pessac, France, and Chemical Biology Team, Biol...
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We report here the details of G4-FID (G-quadruplex fluorescent intercalator displacement), a simple method aiming at evaluating quadruplex-DNA binding affinity and quadruplex- over duplex-DNA selectivity of putative ligands. This assay is based on the loss of fluorescence upon displacement of thiazole orange from quadruplex- and duplex-DNA matrices. The original protocol was tested using variou...
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G-quadruplexes are four-stranded nucleic acid secondary structures that are formed in guanine-rich sequences. G-quadruplexes are widely distributed in functional regions of the human genome and transcriptome, such as human telomeres, oncogene promoter regions, replication initiation sites, and untranslated regions. Many G-quadruplex-forming sequences are found to be associated with cancer, and ...
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A series of G-quadruplex stabilizing compounds have been prepared via click chemistry employing the Cu(I)-catalyzed Huisgen reaction. These compounds were shown to bind tightly to G-quadruplex DNA even in the presence of competing high concentrations of duplex DNA. Furthermore, a modified TRAP assay has shown that some of these compounds also inhibit telomerase at low micromolar concentration.
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2010
ISSN: 0022-2623,1520-4804
DOI: 10.1021/jm1000612