Synthesis and anti-HIV activity of phosphorothioate antisense DNA containing C-5 polyamine substituted 2'-deoxyuridine and/or acridine residues.
Novel phosphorotioate DNAs (S-ODNs) bearing polyamine moiety at the C-5 position of 2'-deoxyuridine in place of certain thymidine residues and/or an acridine moiety at the 5'-terminus were prepared. The sequence of the S-ODNs is complementary to the rev region of HIV-1 mRNA. The duplexes consisted of the modified S-ODNs and the complementary DNA exhibited the enhanced stability compared to that consisted of the corresponding unmodified S-ODN and the complement. The improved antisense activity against HIV-1 was also observed for all modified S-ODNs.
Shinozuka
K
K
Department of Chemistry, Faculty of Engineering, Gunma University, Japan.
Okamoto
T
T
Matsukura
M
M
Sawai
H
H
D000166:Acridines; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D003857:Deoxyuridine; D016679:Genome, Viral; D016655:HIV Core Protein p24 / Q000096:biosynthesis; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D008969:Molecular Sequence Data; D009838:Oligodeoxyribonucleotides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011073:Polyamines; D013873:Thionucleotides
D000166:Acridines; D019380:Anti-HIV Agents; D016655:HIV Core Protein p24; D009838:Oligodeoxyribonucleotides; D011073:Polyamines; D013873:Thionucleotides; D003857:Deoxyuridine