Synthesis of aniline-type analogues of farnesyl diphosphate and their biological assays for prenyl protein transferase inhibitory activity

  • Filippo Minutolo
  • , Simone Bertini
  • , Laura Betti
  • , Valeria Di Bussolo
  • , Gino Giannaccini
  • , Giorgio Placanica
  • , Simona Rapposelli
  • , H. Peter Spielmann
  • , Marco Macchia

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

Abstract

Stable analogues of farnesyl diphosphate, possessing an aniline-type portion in the prenyl-mimic moiety and phosphonoacetamido(oxy) groups in the place of the metabolically unstable diphosphate unit, were synthesised and submitted to biological assays. The enzyme inhibition tests performed on FTase and GGTase I show that the newly synthesised compounds based on a combination of the aniline-containing portions with (phosphonoacetamido)oxy groups do not afford potent inhibitors.

Original languageEnglish
Pages (from-to)1277-1281
Number of pages5
JournalFarmaco
Volume58
Issue number12
DOIs
StatePublished - Dec 2003

Keywords

  • Aniline
  • FTase
  • Farnesyldiphosphate
  • Hexafluoroaniline
  • Phosphonoacetamido(oxy)

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

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