Prenyloxyphenylpropanoids as novel lead compounds for the selective inhibition of geranylgeranyl transferase I
- 作者：Francesco Epifano ; Massimo Curini ; Salvatore Genovese ; Michelle Blaskovich ; Andrew Hamilton ; Said M. Sebti
- 关键词：Prenyloxyphenylpropanoids ; Prenyltransferase ; Coumarins ; Cinnamic acid derivatives ; Anticancer activity
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：1 May 2007
- 卷：17
- 期：9
- 页码：2639-2642
- 文件大小：131 K
摘要
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.