132392-26-8Relevant articles and documents
COMPOUNDS AND METHODS FOR INHIBITING CYP26 ENZYMES
-
, (2018/07/05)
Compounds described herein are inhibitors of retinoic acid inducible P450 (CYP26) enzymes, and are useful for treating diseases that are responsive to retinoids. Certain compounds have retinoid activity, are resistant to CYP26-mediated catabolism, and are used for treating diseases that are responsive to retinoids.
TROPOLONE DERIVATIVE
-
Page/Page column 11, (2010/11/29)
Tropolone derivatives represented by the formula (I), which have retinoid actions and are useful as active ingredients of medicaments [R1 to R4 represent hydrogen atom, an alkyl group, or an alkoxyl group; the ring represented by Ar
A novel type of retinoic acid receptor antagonist: Synthesis and structure-activity relationships of heterocyclic ring-containing benzoic acid derivatives
Yoshimura,Nagai,Hibi,Kikuchi,Abe,Hida,Higashi,Yamanaka
, p. 3163 - 3173 (2007/10/02)
A new series of heterocyclic ring-containing benzoic acids was prepared, and the binding affinity and antagonism of its members against all-trans- retinoic acid were evaluated by in vitro assay systems using human promyelocytic leukemia (HL-60) cells. Structure-activity relationships indicated that both an N-substituted pyrrole or pyrazole (1-position) and a hydrophobic region, with these linked by a ring system, were indispensable for effective antagonism. Among the compounds evaluated, optimal antagonism was exhibited by 4-[4,5,7,8,9,10-hexahydro-7,7,10,-10-tetramethyl-1-(3- pyridylmethyl)anthra[1,2-b]pyrrol-3-yl]benzoic acid (31), 4-[4,5,7,8,9,10- hexahydro-7,7,10,10-tetramethyl-1-(3-pyridylmethyl)-5-thiaanthra[1,2- b]pyrrol-3-yl]benzoic acid (40), and 4-[4,5,7,8,9,10-hexahydro-7,7,10,10- tetramethyl-1-(3-pyridylmethyl)anthra[2,1-d]pyrazol-3-yl]benzoic acid (55), all of which possess a 3-pyridylmethyl group at the five-membered ring nitrogen atom.