title: Synthesis of LIAZAL, a retinoic acid metabolism blocking agent (RAMBA) with potential clinical applications in oncology and dermatology.
abstract: The synthesis of LIAZAL (compound 9, R085246) is described. LIAZAL inhibits all-trans-retinoic acid metabolism and thereby exerts retinoid-like effects in vivo.
authors.affiliation: Department of Medicinal Chemistry, Janssen Research Foundation, Beerse, Belgium. efreyne@janbe.jnj.com
authors.forename: E
authors.initials: E
authors.lastname: Freyne
authors.forename: A
authors.initials: A
authors.lastname: Raeymaekers
authors.forename: M
authors.initials: M
authors.lastname: Venet
authors.forename: G
authors.initials: G
authors.lastname: Sanz
authors.forename: W
authors.initials: W
authors.lastname: Wouters
authors.forename: R
authors.initials: R
authors.lastname: De Coster
authors.forename: J V
authors.initials: JV
authors.lastname: Wauwe
mesh_terms: 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
chemical_list: 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