2. Academic Validation
  3. Design and evaluation of new antipsoriatic antedrug candidates having 16-en-22-oxa-vitamin D3 structures

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

  • Bioorg Med Chem Lett. 2006 Jun 15;16(12):3323-9. doi: 10.1016/j.bmcl.2006.03.014.
Kazuki Shimizu 1,  Akira Kawase,  Tsuyoshi Haneishi,  Yasuharu Kato,  Kazutomo Kinoshita,  Masayuki Ohmori,  Yoshiyuki Furuta,  Takashi Emura,  Nobuaki Kato,  Tetsuya Mitsui,  Koji Yamaguchi,  Keiichi Morita,  Nobuo Sekiguchi,  Tessai Yamamoto,  Tomochika Matsushita,  Shin Shimaoka,  Atsuko Sugita,  Kazumi Morikawa
Affiliations

Affiliation

  • 1 Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd, 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. [email protected]
PMID: 16630723 DOI: 10.1016/j.bmcl.2006.03.014
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).

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