NOVEL C-4 SUBSTITUTED RETINOIDS

摘要

Novel C-4 substituted all-trans retinoic acid analogs are synthesized and used to treat various cancers and dermatological diseases and conditions. These novel C-4 substituted all-trans retinoic acid analogs inhibit all-trans retinoic acid (ATRA) 4-hydroxylase activity, thereby inhibiting the catabolism of ATRA. These novel C-4 substituted ATRA analogs also have ATRA-mimetic activity. The substitutions at C-4 comprise azole, sulfur, oxygen, nitrogen, pyridyl, acetylinic, cyclopropyl-amine, ester, oxime, cyano, oxirone and aziridine groups.