Design and evaluation of new antipsoriatic antedrug candidates having 16-en-22-oxa-vitamin D₃ structures

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• 作者：Kazuki Shimizu ; Akira Kawase ; Tsuyoshi Haneishi ; Yasuharu Kato ; Kazutomo Kinoshita ; Masayuki Ohmori ; Yoshiyuki Furuta ; Takashi Emura ; Nobuaki Kato ; Tetsuya Mitsui et al.
• 关键词：16-En-22-oxa-24-carboalkoxide-1α ; 25-dihydroxyvitamin D₃ analogs ; 16-En-22-oxa-24-carbamide-1α ; 25-dihydroxyvitamin D₃ analogs ; Antedrug ; Low calcemic activity ; Psoriasis
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：15 June 2006
• 年：2006
• 卷：16
• 期：12
• 页码：3323-3329
• 全文大小：215 K

文摘

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).