title: Biologically active oligodeoxyribonucleotides--I: Syntheses and anti-HIV-1 activities of 5'-modified pentadecadeoxyribonucleotides.
abstract: 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.
authors.affiliation: Bioscience Research Laboratories, Sankyo Company Ltd., Tokyo, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Hotoda
authors.forename: K
authors.initials: K
authors.lastname: Momota
authors.forename: H
authors.initials: H
authors.lastname: Furukawa
authors.forename: T
authors.initials: T
authors.lastname: Nakamura
authors.forename: M
authors.initials: M
authors.lastname: Kaneko
authors.forename: S
authors.initials: S
authors.lastname: Kimura
authors.forename: K
authors.initials: K
authors.lastname: Shimada
mesh_terms: 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
chemical_list: D000998:Antiviral Agents; D016376:Oligonucleotides, Antisense; D009943:Organophosphorus Compounds