Design and evaluation of new antipsoriatic antedrug candidates having 16-en-22-oxa-vitamin D3 structures.
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).
Shimizu
Kazuki
K
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd, 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. tazumikzk@chugai-pharm.co.jp
Kawase
Akira
A
Haneishi
Tsuyoshi
T
Kato
Yasuharu
Y
Kinoshita
Kazutomo
K
Ohmori
Masayuki
M
Furuta
Yoshiyuki
Y
Emura
Takashi
T
Kato
Nobuaki
N
Mitsui
Tetsuya
T
Yamaguchi
Koji
K
Morita
Keiichi
K
Sekiguchi
Nobuo
N
Yamamoto
Tessai
T
Matsushita
Tomochika
T
Shimaoka
Shin
S
Sugita
Atsuko
A
Morikawa
Kazumi
K
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
D002762:Cholecalciferol