title: Design and evaluation of new antipsoriatic antedrug candidates having 16-en-22-oxa-vitamin D3 structures.
abstract: Design, synthesis, and in vitro and in vivo evaluation of a series of antipsoriatic antedrugs having 16-en-22-oxa-vitamin D3 are described. Among the seven compounds examined, two are promising: ester 5c and amide 5f, both of which exhibit greater potent antiproliferation activity with lessened calcemic activity than the presently prescribed maxacalcitol (2).
authors.affiliation: Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd, 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. tazumikzk@chugai-pharm.co.jp
authors.forename: Kazuki
authors.initials: K
authors.lastname: Shimizu
authors.forename: Akira
authors.initials: A
authors.lastname: Kawase
authors.forename: Tsuyoshi
authors.initials: T
authors.lastname: Haneishi
authors.forename: Yasuharu
authors.initials: Y
authors.lastname: Kato
authors.forename: Kazutomo
authors.initials: K
authors.lastname: Kinoshita
authors.forename: Masayuki
authors.initials: M
authors.lastname: Ohmori
authors.forename: Yoshiyuki
authors.initials: Y
authors.lastname: Furuta
authors.forename: Takashi
authors.initials: T
authors.lastname: Emura
authors.forename: Nobuaki
authors.initials: N
authors.lastname: Kato
authors.forename: Tetsuya
authors.initials: T
authors.lastname: Mitsui
authors.forename: Koji
authors.initials: K
authors.lastname: Yamaguchi
authors.forename: Keiichi
authors.initials: K
authors.lastname: Morita
authors.forename: Nobuo
authors.initials: N
authors.lastname: Sekiguchi
authors.forename: Tessai
authors.initials: T
authors.lastname: Yamamoto
authors.forename: Tomochika
authors.initials: T
authors.lastname: Matsushita
authors.forename: Shin
authors.initials: S
authors.lastname: Shimaoka
authors.forename: Atsuko
authors.initials: A
authors.lastname: Sugita
authors.forename: Kazumi
authors.initials: K
authors.lastname: Morikawa
mesh_terms: D000818:Animals; D002762:Cholecalciferol / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D015195:Drug Design; D015394:Molecular Structure; D011565:Psoriasis / Q000188:drug therapy*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D002762:Cholecalciferol