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Design and evaluation of new antipsoriatic antedrug candidates having 16-en- 22-oxa-vitamin D sub(3) structures

Design, synthesis, and in vitro and in vivo evaluation of a series of antipsoriatic antedrugs having 16-en-22-oxa-vitamin D sub(3) are described. Among the seven compounds examined, two are promising: ester 5c and amide 5f, both of which exhibit greater potent antiproliferation activity with lessene...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-06, Vol.16 (12), p.3323-3329
Main Authors: Shimizu, Kazuki, Kawase, Akira, Haneishi, Tsuyoshi, Kato, Yasuharu, Kinoshita, Kazutomo, Ohmori, Masayuki, Furuta, Yoshiyuki, Emura, Takashi, Kato, Nobuaki, Mitsui, Tetsuya, Yamaguchi, Koji, Morita, Keiichi, Sekiguchi, Nobuo, Yamamoto, Tessai, Matsushita, Tomochika, Shimaoka, Shin, Sugita, Atsuko, Morikawa, Kazumi
Format: Article
Language:English
Online Access:Get full text
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Summary:Design, synthesis, and in vitro and in vivo evaluation of a series of antipsoriatic antedrugs having 16-en-22-oxa-vitamin D sub(3) 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