Description

• Title:
  SYNTHESIS, BIOLOGICAL PROPERTIES AND ANTI-HIV-1 ACTIVITY OF NEW PYRIMIDINE P1,P2-DINUCLEOTIDES
• Creator:
  Miazga, Agnieszka;
  Ziemkowski, Przemysław;
  Siwecka, Maria;
  Lipniacki, Andrzej;
  Piasek, Andrzej;
  Kulikowski, Tadeusz
• Description:
  New homo- and hetero-P1,P2-dinucleotides were prepared with the use of multistep procedures starting from the monophosphates of 3'-fluoro-2-thiothymidine, 3'-fluoro-4-thiothymidine, AZT and 1-[(2-hydroxyethoxy)-methyl-5-propyl-6-phenylselenenyl]uracil. Anti-HIV properties of the synthesized P1,P2-dinucleotides were evaluated against laboratory syncytia inducing strain HIV-1 in CEM-T4 cells. Anti-HIV activities were in the range of 5–45 nM, and therapeutic indexes were higher than 4666–14000. Interactions of the above mentioned compounds with recombinant HIV-1 reverse transcriptase were also investigated. The obtained results point to reverse transcriptase inhibition, with somewhat lower inhibitory activity than that of their parental nucleoside-5'-triphosphates. Compound 6 may be regarded as a potent anti-HIV/AIDS drug.
• Object availability:
  free access
• Date:
  2010
• Type:
  Article;
  PeerReviewed
• Language:
  English
• Format:
  application/pdf
• Publisher:
  Taylor and Francis Group
• Relation: http://eprints.ibb.waw.pl/40 ;
  ISSN: 1525-7770 print / 1532-2335 online
• Subject:
  QD Chemistry;
  QR355 Virology
• Identifier: http://eprints.ibb.waw.pl/40/1/nnn_2010_438.pdf ;
  Miazga, Agnieszka and Ziemkowski, Przemysław and Siwecka, Maria and Lipniacki, Andrzej and Piasek, Andrzej and Kulikowski, Tadeusz (2010) SYNTHESIS, BIOLOGICAL PROPERTIES AND ANTI-HIV-1 ACTIVITY OF NEW PYRIMIDINE P1,P2-DINUCLEOTIDES. Nucleosides, Nucleotides and Nucleic Acids, 29 . pp. 438-444.
• Data provider:
  Repozytorium Instytutu Biochemii i Biofizyki Polskiej Akademii Nauk
• Can I use it?:
  seek permission
• Type:
  other