Potent inhibitors of the hedgehog signaling pathway.
A small family of phenyl quinazolinone ureas is reported as potent modulators of Hedgehog protein function. Preliminary SAR studies of the urea substituent led to a nanomolar Hedgehog antagonist.
Brunton
Shirley A
SA
Evotec, Oxfordshire, UK. shirley.brunton@evotec.com
Stibbard
John H A
JH
Rubin
Lee L
LL
Kruse
Lawrence I
LI
Guicherit
Oivin M
OM
Boyd
Edward A
EA
Price
Steven
S
D000818:Animals; D002460:Cell Line; D053823:Hedgehog Proteins / Q000037:antagonists & inhibitors* / Q000502:physiology; D051379:Mice; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015398:Signal Transduction; D013329:Structure-Activity Relationship
D053823:Hedgehog Proteins; D052999:Quinazolinones