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Bioorg Med Chem Lett. 2004 Feb 9;14(3):639-43.

Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. christopher_dinsmore@merck.com

Abstract

A series of macrocyclic piperazinone compounds with dual farnesyltransferase/geranylgeranyltransferase-I inhibitory activity was prepared. These compounds were found to be potent inhibitors of protein prenylation in cell culture. A hypothesis for the binding mode of compound 3o in FPTase is proposed.

PMID:
14741259
DOI:
10.1016/j.bmcl.2003.11.051
[Indexed for MEDLINE]

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