Potent, non-thiol inhibitors of farnesyltransferase

M J Breslin; S J deSolms; E A Giuliani; G E Stokker; S L Graham; D L Pompliano; S D Mosser; K A Hamilton; J H Hutchinson

doi:10.1016/s0960-894x(98)00586-1

Potent, non-thiol inhibitors of farnesyltransferase

Bioorg Med Chem Lett. 1998 Dec 1;8(23):3311-6. doi: 10.1016/s0960-894x(98)00586-1.

Authors

M J Breslin¹, S J deSolms, E A Giuliani, G E Stokker, S L Graham, D L Pompliano, S D Mosser, K A Hamilton, J H Hutchinson

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.

PMID: 9873725
DOI: 10.1016/s0960-894x(98)00586-1

Abstract

The structure-activity relationship of a series of non-thiol CaaX analogs, which are inhibitors of farnesyltransferase, is described. These inhibitors contain a substituted phenyl group at the N terminus, which may occupy a novel binding domain on the Ras protein.

MeSH terms

Alkyl and Aryl Transferases / antagonists & inhibitors*
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Farnesyltranstransferase
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Alkyl and Aryl Transferases
Farnesyltranstransferase