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

doi:10.1016/j.bmcl.2007.01.097

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

Chemistry

Research output: Contribution to journal › Article › peer-review

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 language	English (US)
Pages (from-to)	2639-2642
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	9
DOIs	https://doi.org/10.1016/j.bmcl.2007.01.097
State	Published - 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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10.1016/j.bmcl.2007.01.097

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title = "Prenyloxyphenylpropanoids as novel lead compounds for the selective inhibition of geranylgeranyl transferase I",

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.",

keywords = "Anticancer activity, Cinnamic acid derivatives, Coumarins, Prenyloxyphenylpropanoids, Prenyltransferase",

author = "Francesco Epifano and Massimo Curini and Salvatore Genovese and Michelle Blaskovich and Andrew Hamilton and Sebti, {Said M.}",

note = "Funding Information: Authors from Italy wish to acknowledge financial support from MIUR (Rome, Italy) National Project {\textquoteleft}Sviluppo di processi sintetici ecocompatibili nella sintesi organica{\textquoteright}, COFIN 2004.",

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doi = "10.1016/j.bmcl.2007.01.097",

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AU - Epifano, Francesco

AU - Curini, Massimo

AU - Genovese, Salvatore

AU - Blaskovich, Michelle

AU - Hamilton, Andrew

AU - Sebti, Said M.

N1 - Funding Information: Authors from Italy wish to acknowledge financial support from MIUR (Rome, Italy) National Project ‘Sviluppo di processi sintetici ecocompatibili nella sintesi organica’, COFIN 2004.

PY - 2007/5/1

Y1 - 2007/5/1

N2 - 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.

AB - 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.

KW - Anticancer activity

KW - Cinnamic acid derivatives

KW - Coumarins

KW - Prenyloxyphenylpropanoids

KW - Prenyltransferase

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JO - Bioorganic and Medicinal Chemistry Letters

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ER -

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

Abstract

Keywords

ASJC Scopus subject areas

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