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
  • Farnesyldiphosphate
  • FTase
  • Hexafluoroaniline
  • Phosphonoacetamido(oxy)

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

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