Biologically active oligodeoxyribonucleotides--I: Syntheses and anti-HIV-1 activities of 5'-modified pentadecadeoxyribonucleotides.
5'-Modified pentadecadeoxyribonucleotides with a sequence (5'-TGGGAGGTGGGTCTG-3') (15mer) complimentary (antisense) 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 modified antisense oligodeoxyribonucleotides (AS-ODNs) were synthesized using 5'-modified thymidine 3'-phosphoramidites as the 5'-terminal residues. The structures of the 5'-modified 15mers were confirmed by negative ion LSI mass spectroscopy, and the anti-HIV-1 activities were evaluated in vitro by the 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 high anti-HIV-1 activities.
Hotoda
H
H
Bioscience Research Laboratories, Sankyo Company Ltd., Tokyo, Japan.
Momota
K
K
Furukawa
H
H
Nakamura
T
T
Kaneko
M
M
Kimura
S
S
Shimada
K
K
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001483:Base Sequence; D002478:Cells, Cultured; D015756:Genes, tat; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D008969:Molecular Sequence Data; D016376:Oligonucleotides, Antisense / Q000138:chemical synthesis* / Q000235:genetics / Q000494:pharmacology; D009943:Organophosphorus Compounds / Q000737:chemistry
D000998:Antiviral Agents; D016376:Oligonucleotides, Antisense; D009943:Organophosphorus Compounds