Novel series of [ddN]-[TSAO-T] heterodimers as potential bi-functional inhibitors of HIV-1 RT. Studies in the linker and ddN region

Nucleosides Nucleotides. 1999 Apr-May;18(4-5):1029-30. doi: 10.1080/15257779908041640.

Abstract

Novel series of [ddN]-(CH2)n-[TSAO-T] heterodimers have been prepared and tested for their anti-HIV-1 and HIV-2 activity. The most active compound of this series was the [d4T]-(CH2)3-[TSAO-T] heterodimer (EC50 = 0.018 +/- 0.03 microM).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Cell Line
  • Dimerization
  • HIV Reverse Transcriptase / antagonists & inhibitors
  • HIV-1 / drug effects
  • HIV-1 / enzymology
  • Humans
  • Reverse Transcriptase Inhibitors / chemistry*
  • Reverse Transcriptase Inhibitors / pharmacology*
  • Spiro Compounds / chemistry*
  • Spiro Compounds / pharmacology*
  • Thymidine / analogs & derivatives*
  • Thymidine / chemistry
  • Thymidine / pharmacology
  • Uridine / analogs & derivatives

Substances

  • Anti-HIV Agents
  • Reverse Transcriptase Inhibitors
  • Spiro Compounds
  • HIV Reverse Transcriptase
  • Thymidine
  • TSAO-T
  • Uridine