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
  • 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).