3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid as a highly potent and selective retinoic acid metabolic blocking agent.
3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid and analogs were designed and synthesized as highly potent and selective CYP26 inhibitors, serving as retinoic acid metabolic blocking agents (RAMBAs), with demonstrated in vivo efficacy to increase the half-life of exogenous atRA.
Mulvihill
Mark J
MJ
OSI Pharmaceuticals, Inc., 1 Bioscience Park Drive, Farmingdale, NY 11735, USA. mmulvihill@osip.com
Kan
Julie L C
JL
Cooke
Andrew
A
Bhagwat
Shripad
S
Beck
Patricia
P
Bittner
Mark
M
Cesario
Cara
C
Keane
David
D
Lazarescu
Viorica
V
Nigro
Anthony
A
Nillson
Christy
C
Panicker
Bijoy
B
Smith
Vanessa
V
Srebernak
Mary
M
Sun
Feng-Lei
FL
O'Connor
Matthew
M
Russo
Suzanne
S
Fischetti
Gia
G
Vrkljan
Michael
M
Winski
Shannon
S
Castelhano
Arlindo L
AL
Emerson
David
D
Gibson
Neil W
NW
D002851:Chromatography, High Pressure Liquid; D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System; D004791:Enzyme Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology*; D006207:Half-Life; D013058:Mass Spectrometry; D009281:Naphthalenes / Q000493:pharmacokinetics / Q000494:pharmacology*; D011422:Propionates / Q000493:pharmacokinetics / Q000494:pharmacology*; D000072516:Retinoic Acid 4-Hydroxylase; D014212:Tretinoin / Q000037:antagonists & inhibitors / Q000378:metabolism*
C512307:3-(6-(2-dimethylamino-1-imidazol-1-yl-butyl)naphthalen-2-yloxy)-2,2-dimethyl-propionic acid; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D009281:Naphthalenes; D011422:Propionates; D014212:Tretinoin; D003577:Cytochrome P-450 Enzyme System; D000072516:Retinoic Acid 4-Hydroxylase