5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.
The evaluation of structure-activity relationships associated with the modification of the R115777 quinolinone ring moiety displaying potent in vitro inhibiting activity is described.
Angibaud
Patrick
P
Medicinal Chemistry Department, Johnson & Johnson Pharmaceutical Research & Development, Campus de Maigremont BP615, 27106 Val de Reuil, France. pangibau@prdfr.jnj.com
Bourdrez
Xavier
X
Devine
Ann
A
End
David W
DW
Freyne
Eddy
E
Ligny
Yannick
Y
Muller
Philippe
P
Mannens
Geert
G
Pilatte
Isabelle
I
Poncelet
Virginie
V
Skrzat
Stacy
S
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; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001381:Azepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051231:Farnesyltranstransferase; D006801:Humans; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D051379:Mice; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays
D000970:Antineoplastic Agents; D001381:Azepines; D007202:Indicators and Reagents; D011799:Quinazolines; D015363:Quinolones; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase; C402769:tipifarnib