Synthesis and anti-HIV activity of thymidine analogues bearing a 4'-cyanovinyl group and some derivatives thereof

Nucleosides Nucleotides Nucleic Acids. 2001 Dec;20(12):1927-39. doi: 10.1081/NCN-100108323.

Abstract

Treatment of 3'-O-tert-butyldimethylsilyl-2',5'-dideoxy-5'-oxothymidine (4) with potassium or magnesium nitromethanide afforded in good yield the resolvable epimeric mixture of the expected blocked nitronucleosides 5 which upon dehydration led to the corresponding E-nitroenofuranosylthymidine 6. Nucleophilic attack of cyanide onto the nitrovinyl group led to a nucleoside analogue bearing a terminal 1-cyanovinyl group (7), a soft electrophilic group which, upon reaction with benzeneselenol, underwent a conjugate addition to the phenylselenonucleoside derivative 9. All these compounds, eventually de-O-silylated, were subject of in vitro biological testing, some exhibiting interesting cytotoxic or antiviral properties.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / pharmacology*
  • Biochemistry / methods
  • Cell Division / drug effects
  • Drug Evaluation, Preclinical
  • Humans
  • Inhibitory Concentration 50
  • Mice
  • Microbial Sensitivity Tests
  • Silanes / chemical synthesis
  • Silanes / pharmacology*
  • Structure-Activity Relationship
  • Thymidine / analogs & derivatives
  • Thymidine / chemical synthesis
  • Thymidine / chemistry*
  • Thymidine / pharmacology*
  • Tumor Cells, Cultured

Substances

  • 3'-O-tert-butyldimethylsilyl-2',5'-dideoxy-5'-oxothymidine
  • Anti-HIV Agents
  • Silanes
  • Thymidine