3-Aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrrole, a novel class of farnesyltransferase inhibitors.
Design, synthesis and structure-activity relationship of a class of 3-aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrroles as farnesyltransferase inhibitors are described. Compound 7 inhibits farnesyltransferase with an IC(50) value of 4.6 nM.
Lee
H
H
Life Science R & D, LGCI, Science Town, Taejon 305-380, South Korea.
Lee
J
J
Shin
Y
Y
Jung
W
W
Kim
J H
JH
Park
K
K
Ro
S
S
Chung
H H
HH
Koh
J S
JS
D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D051231:Farnesyltranstransferase; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
C443752:3-aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrrole; D004791:Enzyme Inhibitors; D007093:Imidazoles; D011758:Pyrroles; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase