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

Basic Information

ID: ALA1139158

Journal: Bioorg Med Chem Lett

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

Authors: Epifano F, Curini M, Genovese S, Blaskovich M, Hamilton A, Sebti SM.

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 IC(50) values ranging from 28 to 39 microM.

CiteXplore: 17314046

DOI: 10.1016/j.bmcl.2007.01.097

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