Synthesis of a Potent G-Quadruplex-Binding Macrocyclic Heptaoxazole

Synthesis of a Potent G-Quadruplex-Binding Macrocyclic Heptaoxazole

A novel G-quadruplex binder, L1H1-7OTD (shown in color by atom type), was developed. This macrocyclic heptaoxazole potently and selectively stabilizes telomeric DNA in an intramolecular antiparallel G-quadruplex conformation. L1H1-7OTD shows selective cytotoxicity toward HeLa cells, a telomerase-pos...

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Veröffentlicht in:Chembiochem : a European journal of chemical biology 2009-02, Vol.10 (3), p.431-435
Hauptverfasser: Tera, Masayuki, Iida, Keisuke, Ishizuka, Hiromichi, Takagi, Motoki, Suganuma, Masami, Doi, Takayuki, Shin-ya, Kazuo, Nagasawa, Kazuo
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Cell Line
G-Quadruplexes
Humans
macrocycles
Macrocyclic Compounds - chemical synthesis
Macrocyclic Compounds - chemistry
Models, Molecular
Molecular Structure
Nucleic Acid Conformation
Oxazoles - chemical synthesis
Oxazoles - chemistry
polyoxazoles
telomerase inhibitors
Telomere - chemistry
Telomere - genetics
telomeres
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Zusammenfassung:A novel G-quadruplex binder, L1H1-7OTD (shown in color by atom type), was developed. This macrocyclic heptaoxazole potently and selectively stabilizes telomeric DNA in an intramolecular antiparallel G-quadruplex conformation. L1H1-7OTD shows selective cytotoxicity toward HeLa cells, a telomerase-positive cell line.
ISSN:1439-4227
1439-7633
DOI:10.1002/cbic.200800563