2. Academic Validation
  3. Synthesis and antiviral activity of monofluoro and difluoro analogues of pyrimidine deoxyribonucleosides against human immunodeficiency virus (HIV-1)

Synthesis and antiviral activity of monofluoro and difluoro analogues of pyrimidine deoxyribonucleosides against human immunodeficiency virus (HIV-1)

  • J Med Chem. 1990 Aug;33(8):2137-45. doi: 10.1021/jm00170a015.
J A Martin 1,  D J Bushnell,  I B Duncan,  S J Dunsdon,  M J Hall,  P J Machin,  J H Merrett,  K E Parkes,  N A Roberts,  G J Thomas
Affiliations

Affiliation

  • 1 Research Division, Roche Products Limited, Welwyn Garden City, Hertfordshire, England.
PMID: 2165161 DOI: 10.1021/jm00170a015
Abstract

A range of 2'-fluoro and 2',3'-difluoro analogues of pyrimidine deoxyribonucleosides have been synthesized and evaluated against human immunodeficiency virus (HIV-1) in a human lymphoblastoid cell line. Among these compounds, 1-(2,3-dideoxy-2-fluoro-beta-D-threopentofuranosyl)cytosine (12), 2',3'-didehydro-2',3'-dideoxy-2'-fluorocytidine (35), 1-(2,3-dideoxy-2,3-difluoro-beta-D-arabinofuranosyl)cytosine (41), and 3'-deoxy-2',3'-didehydro-2'-fluorothymidine (45) were found to have significant Antiviral activity, with IC50 values of 0.65, 10, 10, and 100 microM, respectively. The structure-activity relationships are discussed.

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