Potent, non-thiol inhibitors of farnesyltransferase.
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.
Breslin
M J
MJ
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.
deSolms
S J
SJ
Giuliani
E A
EA
Stokker
G E
GE
Graham
S L
SL
Pompliano
D L
DL
Mosser
S D
SD
Hamilton
K A
KA
Hutchinson
J H
JH
D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051231:Farnesyltranstransferase; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase