Synthesis of a Potent G-Quadruplex-Binding Macrocyclic Heptaoxazole

Authors

  • Masayuki Tera,

    1. Department of Biotechnology and Life Science, Faculty of Technology, Tokyo University of Agriculture and Technology (TUAT), 2-24-16 Nakamachi, Koganei Tokyo 184-8588 (Japan), Fax: (+81) 42-388-7295
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  • Keisuke Iida,

    1. Department of Biotechnology and Life Science, Faculty of Technology, Tokyo University of Agriculture and Technology (TUAT), 2-24-16 Nakamachi, Koganei Tokyo 184-8588 (Japan), Fax: (+81) 42-388-7295
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  • Hiromichi Ishizuka,

    1. Department of Biotechnology and Life Science, Faculty of Technology, Tokyo University of Agriculture and Technology (TUAT), 2-24-16 Nakamachi, Koganei Tokyo 184-8588 (Japan), Fax: (+81) 42-388-7295
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  • Motoki Takagi Dr.,

    1. Biomedicinal Information Research Center (BIRC), Japan Biological Informatics Consortium (JBIC), Koto-ku, Tokyo 135-0064 (Japan)
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  • Masami Suganuma Dr.,

    1. Research Institute for Clinical Oncology, Saitama Cancer Center, Ina, Kitaadachi-gun, Saitama 362-0806 (Japan)
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  • Takayuki Doi Prof. Dr.,

    1. Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba, Aramaki, Aoba-ku, Sendai, Miyagi 980-8578 (Japan)
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  • Kazuo Shin-ya Dr.,

    1. Biological Information Research Center, National Institute of Advanced Industrial Science and Technology (AIST), Koto-ku, Tokyo 135-0064 (Japan)
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  • Kazuo Nagasawa Prof. Dr.

    1. Department of Biotechnology and Life Science, Faculty of Technology, Tokyo University of Agriculture and Technology (TUAT), 2-24-16 Nakamachi, Koganei Tokyo 184-8588 (Japan), Fax: (+81) 42-388-7295
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Abstract

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.

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