Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.
A series of (4-chlorophenyl)-alpha-(1-methyl-1H-imidazol-5-yl)azoloquinolines and -quinazolines was prepared. These compounds displayed potent Farnesyl Protein Transferase inhibitory activity and tetrazolo[1,5-a]quinazolines are promising agents for oral in vivo inhibition.
Angibaud
Patrick
P
Medicinal Chemistry Department Johnson & Johnson Pharmaceutical Research & Development (J&JPRD), Campus de Maigremont BP615, 27106, Val de Reuil, France. pangibau@prdfr.jnj.com
Bourdrez
Xavier
X
End
David W
DW
Freyne
Eddy
E
Janicot
Michel
M
Lezouret
Patricia
P
Ligny
Yannick
Y
Mannens
Geert
G
Damsch
Siegrid
S
Mevellec
Laurence
L
Meyer
Christophe
C
Muller
Philippe
P
Pilatte
Isabelle
I
Poncelet
Virginie
V
Roux
Bruno
B
Smets
Gerda
G
Van Dun
Jacky
J
Van Remoortere
Pieter
P
Venet
Marc
M
Wouters
Walter
W
D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D000818:Animals; D002455:Cell Division / Q000187:drug effects; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D051231:Farnesyltranstransferase; D007700:Kinetics; D008968:Molecular Conformation; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D011799:Quinazolines; D011804:Quinolines; D015363:Quinolones; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase; C402769:tipifarnib