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-positive cell line.
Tera
Masayuki
M
Department of Biotechnology and Life Science, Faculty of Technology, Tokyo University of Agriculture and Technology, Koganei, Tokyo, Japan.
Iida
Keisuke
K
Ishizuka
Hiromichi
H
Takagi
Motoki
M
Suganuma
Masami
M
Doi
Takayuki
T
Shin-ya
Kazuo
K
Nagasawa
Kazuo
K
D000818:Animals; D002460:Cell Line; D054856:G-Quadruplexes; D006801:Humans; D047028:Macrocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D008958:Models, Molecular; D015394:Molecular Structure; D009690:Nucleic Acid Conformation; D010080:Oxazoles / Q000138:chemical synthesis* / Q000737:chemistry; D016615:Telomere / Q000737:chemistry / Q000235:genetics
D047028:Macrocyclic Compounds; D010080:Oxazoles