Prenyloxyphenylpropanoids as novel lead compounds for the selective inhibition of geranylgeranyl transferase I

Francesco Epifano, Massimo Curini, Salvatore Genovese, Michelle Blaskovich, Andrew Hamilton, Said M. Sebti

Research output: Contribution to journalArticle

Abstract

In this study, we synthesized some natural and semisynthetic prenyloxyphenylpropanoids (e.g., coumarins and cinnamic acid derivatives) and we assessed their in vitro inhibitory activity against farnesyl transferase (FTase) and geranylgeranyl transferase I (GGTase I). No compound was an effective inhibitor of FTase, while farnesyloxycinnamic acids were shown to selectively inhibit GGTase I with IC50 values ranging from 28 to 39 μM.

Original languageEnglish (US)
Pages (from-to)2639-2642
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number9
DOIs
StatePublished - May 1 2007

Keywords

  • Anticancer activity
  • Cinnamic acid derivatives
  • Coumarins
  • Prenyloxyphenylpropanoids
  • Prenyltransferase

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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