Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation.
Farnesyltransferase inhibitors (FTIs) have been developed as potential anti-cancer agents due to their efficacy in blocking malignant growth in a variety of murine models of human tumors. To that end, we have developed a series of pyridone farnesyltransferase inhibitors with potent in vitro and cellular activity. The synthesis, SAR and biological properties of these compounds will be discussed.
Pharmaceutical Discovery, R-47B, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6101, USA. lisa.hasvold@abbott.com
Lisa A
LA
Hasvold
Weibo
W
Wang
Stephen L
SL
Gwaltney
Todd W
TW
Rockway
Lissa T J
LT
Nelson
Robert A
RA
Mantei
Stephen A
SA
Fakhoury
Gerard M
GM
Sullivan
Qun
Q
Li
Nan-Horng
NH
Lin
Le
L
Wang
Haiying
H
Zhang
Jerome
J
Cohen
Wen-Zhen
WZ
Gu
Kennan
K
Marsh
Joy
J
Bauch
Saul
S
Rosenberg
Hing L
HL
Sham
D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000633:toxicity; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000633:toxicity; D051231:Farnesyltranstransferase; D006801:Humans; D015394:Molecular Structure; D011728:Pyridones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011728:Pyridones; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase