2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase

Authors
Trotter, BW Quigley, AG Lumma, WC Sisko, JT Walsh, ES Hamann, CS Robinson, RG Bhimnathwala, H Kolodin, DG Zheng, W Buser, CA Huber, HE Lobell, RB Kohl, NE Williams, TM Graham, SL Dinsmore, CJ
Citation
Bw. Trotter et al., 2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase, BIOORG MED, 11(7), 2001, pp. 865-869
Citations number
24
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
7
Year of publication
2001
Pages
865 - 869
Database
ISI
SICI code
0960-894X(20010409)11:7<865:2FIOFP>2.0.ZU;2-B
Abstract
A series of 2-arylindole-3-acetamide farnesyl protein transferase inhibitor s has been identified. The compounds inhibit the enzyme in a farnesyl pyrop hosphate-competitive manner and are selective for farnesyl protein transfer ase over the related enzyme geranylgeranyltransferase-I. A representative m ember of this series of inhibitors demonstrates equal effectiveness against HDJ-2 and K-Ras farnesylation in a cell-based assay when geranylgeranylati on is suppressed. (C) 2001 Published by Elsevier Science Ltd.