(-)-2'-deoxy-3'-thiacytidine is a potent, highly selective inhibitor of human immunodeficiency virus type 1 and type 2 replication in vitro

Antimicrob Agents Chemother. 1992 Apr;36(4):733-9. doi: 10.1128/AAC.36.4.733.


The (-)-enantiomer of 2'-deoxy-3'-thiacytidine (3TC) was found to be a potent and selective inhibitor of human immunodeficiency virus types 1 (HIV-1) and 2 (HIV-2) in vitro. We determined its antiviral activity against a number of laboratory strains of HIV-1 and HIV-2 in a range of CD4-bearing lymphocyte cell lines (mean 50% inhibitory concentration [IC50] range, 4 nM to 0.67 microM). 3TC was also active against a range of HIV-1 strains in peripheral blood lymphocytes (mean IC50 range, 2.5 to 90 nM). The IC50 for cytotoxicity in seven lymphocyte cell cultures, including human peripheral blood lymphocytes, ranged from 0.5 to 6 mM. 3TC had no detectable antiviral activity against a range of other viruses or in cells chronically infected with HIV-1 or HIV-2. The effects of time of addition of the compound and varying the multiplicity of infection on the antiviral activity of 3TC were determined. The results showed that 3TC is a potent and selective inhibitor of HIV-1 and HIV-2 replication in vitro.

Publication types

  • Comparative Study

MeSH terms

  • Cell Death / drug effects
  • Cells, Cultured
  • Didanosine / pharmacology
  • Giant Cells / drug effects
  • HIV Reverse Transcriptase
  • HIV-1 / drug effects*
  • HIV-2 / drug effects*
  • Humans
  • Lamivudine
  • RNA-Directed DNA Polymerase / analysis
  • Tritium
  • Virus Replication / drug effects
  • Zalcitabine / analogs & derivatives*
  • Zalcitabine / pharmacology
  • Zidovudine / pharmacology


  • Tritium
  • Lamivudine
  • Zidovudine
  • Zalcitabine
  • HIV Reverse Transcriptase
  • RNA-Directed DNA Polymerase
  • Didanosine