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 calc...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-06, Vol.16 (12), p.3323-3329
Hauptverfasser:	SHIMIZU, Kazuki, KAWASE, Akira, YAMAGUCHI, Koji, MORITA, Keiichi, SEKIGUCHI, Nobuo, YAMAMOTO, Tessai, MATSUSHITA, Tomochika, SHIMAOKA, Shin, SUGITA, Atsuko, MORIKAWA, Kazumi, HANEISHI, Tsuyoshi, KATO, Yasuharu, KINOSHITA, Kazutomo, OHMORI, Masayuki, FURUTA, Yoshiyuki, EMURA, Takashi, KATO, Nobuaki, MITSUI, Tetsuya
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Cholecalciferol - chemical synthesis Cholecalciferol - chemistry Cholecalciferol - pharmacology Cholecalciferol - therapeutic use Drug Design Medical sciences Molecular Structure Pharmacology. Drug treatments Psoriasis - drug therapy Rats Skin, nail, hair, dermoskeleton Structure-Activity Relationship
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Zusammenfassung:	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).
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.03.014