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

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.

Graphical abstractThe synthesis of some natural and semisynthetic prenyloxyphenylpropanoids and their selective inhibitory activity on geranylgeranyl transferase I are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide