Synthesis of LIAZAL, a retinoic acid metabolism blocking agent (RAMBA) with potential clinical applications in oncology and dermatology.
The synthesis of LIAZAL (compound 9, R085246) is described. LIAZAL inhibits all-trans-retinoic acid metabolism and thereby exerts retinoid-like effects in vivo.
Freyne
E
E
Department of Medicinal Chemistry, Janssen Research Foundation, Beerse, Belgium. efreyne@janbe.jnj.com
Raeymaekers
A
A
Venet
M
M
Sanz
G
G
Wouters
W
W
De Coster
R
R
Wauwe
J V
JV
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System; D003879:Dermatologic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D051381:Rats; D000072516:Retinoic Acid 4-Hydroxylase; D014212:Tretinoin / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000970:Antineoplastic Agents; D065607:Cytochrome P-450 Enzyme Inhibitors; D003879:Dermatologic Agents; D004791:Enzyme Inhibitors; D007093:Imidazoles; D014212:Tretinoin; D003577:Cytochrome P-450 Enzyme System; D000072516:Retinoic Acid 4-Hydroxylase; C061121:liarozole