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

Fingerprint

Lead compounds
Transferases
Coumarins
Inhibitory Concentration 50
Derivatives
Acids
geranylgeranyltransferase type-I

Keywords

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

ASJC Scopus subject areas

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

Cite this

Prenyloxyphenylpropanoids as novel lead compounds for the selective inhibition of geranylgeranyl transferase I. / Epifano, Francesco; Curini, Massimo; Genovese, Salvatore; Blaskovich, Michelle; Hamilton, Andrew; Sebti, Said M.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 17, No. 9, 01.05.2007, p. 2639-2642.

Research output: Contribution to journalArticle

Epifano, Francesco ; Curini, Massimo ; Genovese, Salvatore ; Blaskovich, Michelle ; Hamilton, Andrew ; Sebti, Said M. / Prenyloxyphenylpropanoids as novel lead compounds for the selective inhibition of geranylgeranyl transferase I. In: Bioorganic and Medicinal Chemistry Letters. 2007 ; Vol. 17, No. 9. pp. 2639-2642.
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