Biologically Active Oligodeoxyribonucleotides. VII. Anti-HIV-1 Activity of Hexadeoxyribonucleotides Bearing 3′- and 5′-End-Modifications

Makoto Koizumi Exploratory Chemistry Research Lab., Sankyo Co., LTD., 1-2-58, Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Rika Koga Exploratory Chemistry Research Lab., Sankyo Co., LTD., 1-2-58, Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Hitoshi Hotoda Exploratory Chemistry Research Lab., Sankyo Co., LTD., 1-2-58, Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Kenji Momota Biological Research Lab., Sankyo Co., LTD., 1-2-58, Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Toshinori Ohmine Biological Research Lab., Sankyo Co., LTD., 1-2-58, Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Hidehiko Furukawa Biological Research Lab., Sankyo Co., LTD., 1-2-58, Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Takashi Nishigakit Biological Research Lab., Sankyo Co., LTD., 1-2-58, Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Koji Abe Analytical and Metabolic Research Lab., Sankyo Co., LTD., 1-2-58, Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Toshiyuki Kosaka Analytical and Metabolic Research Lab., Sankyo Co., LTD., 1-2-58, Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Masakatsu Kaneko Exploratory Chemistry Research Lab., Sankyo Co., LTD., 1-2-58, Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Satoshi Kimura Department of Infectious Diseases, Institute of Medical Science, University of Tokyo, 4-6-1 Shirokanedai, Minato-ku, Tokyo, 108, Japan; Department of Infection Control and Prevention, the University of Tokyo Hospital, 7-3-1, Hongou, Bunkyo-ku, Tokyo, 113, Japan

Kaoru Shimada Department of Infectious Diseases, Institute of Medical Science, University of Tokyo, 4-6-1 Shirokanedai, Minato-ku, Tokyo, 108, Japan; Tokyo Senbai Hospital, 1-4-3, Mita, Minato-ku, Tokyo, 108, Japan

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Abstract

It has been determined that hexadeoxyribonucleotides (5′TGGGAG3′), which have modified aromatic groups such as the trityl group at the 5′-end, exhibit anti-HIV-1 activity in vitro. The 6-mer (S-1443) bearing a 3,4-dibenzyloxybenzyl (3,4-DBB) group at the 5′-end and a 2-hydroxyethylphosphate group at the 3′end exhibited the most potent activity and the least cytotoxicity. Moreover, it was found that the S-1443 was the most stable, when the 6-mer analogues were incubated with mouse, rat, or human plasma.

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Biologically Active Oligodeoxyribonucleotides. VII. Anti-HIV-1 Activity of Hexadeoxyribonucleotides Bearing 3′- and 5′-End-Modifications

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Biologically Active Oligodeoxyribonucleotides. VII. Anti-HIV-1 Activity of Hexadeoxyribonucleotides Bearing 3′- and 5′-End-Modifications

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