Biologically Active Oligodeoxyribonucleotides - II¹: Structure Activity Relationships of Anti-HIV-1 Pentadecadeoxyribonucleotides Bearing 5′-End-Modifications

Hitoshi Hotoda Exploratory Chemistry Research Laboratories, 1-2-58 Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Kenji Momota Biological Research Laboratories, 1-2-58 Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Hidehiko Furukawa Biological Research Laboratories, 1-2-58 Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Takemichi Nakamura Analytical and Metabolic Research Laboratories, Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Masakatsu Kaneko Exploratory Chemistry Research Laboratories, 1-2-58 Hiromachi, Shinagawa-ku, Tokyo, 140, Japan

Satcshi Kimura The Department of Infectious Diseases, the Institute of Medical Science, the University of Tokyo, 4-6-1 Shirokanedai, Minato-ku, Tokyo, 108, Japan

Kawu Shimada The Department of Infectious Diseases, the Institute of Medical Science, the University of Tokyo, 4-6-1 Shirokanedai, Minato-ku, Tokyo, 108, Japan

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Abstract

5′-End-modified pentadecadeoxyribonucleotides (15mers) with a sequence complementary to the tat 2nd splicing acceptor region of human immunodeficiency virus type 1 (HIV-1) were prepared and evaluated for anti-HIV-1 activity. The structures of modified 15mers were confirmed by negative ion LSI mass spectroscopy, and the anti-HIV-1 activities were evaluated in vitro by MTT assay using MT-4 cells. While the unmodified 15mer had no activity in our assay system, the 15mers bearing modifications with trityl-type substituents at the 5′-end showed potent anti-HIV-1 activities.

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Biologically Active Oligodeoxyribonucleotides - II¹: Structure Activity Relationships of Anti-HIV-1 Pentadecadeoxyribonucleotides Bearing 5′-End-Modifications

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Biologically Active Oligodeoxyribonucleotides - II1: Structure Activity Relationships of Anti-HIV-1 Pentadecadeoxyribonucleotides Bearing 5′-End-Modifications

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Biologically Active Oligodeoxyribonucleotides - II¹: Structure Activity Relationships of Anti-HIV-1 Pentadecadeoxyribonucleotides Bearing 5′-End-Modifications