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Bioorg Med Chem Lett. 2001 Apr 9;11(7):865-9.

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

Author information

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

Abstract

A series of 2-arylindole-3-acetamide farnesyl protein transferase inhibitors has been identified. The compounds inhibit the enzyme in a farnesyl pyrophosphate-competitive manner and are selective for farnesyl protein transferase over the related enzyme geranylgeranyltransferase-I. A representative member of this series of inhibitors demonstrates equal effectiveness against HDJ-2 and K-Ras farnesylation in a cell-based assay when geranylgeranylation is suppressed.

PMID:
11294379
DOI:
10.1016/s0960-894x(01)00061-0
[Indexed for MEDLINE]

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