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Paper | Special issue | Vol 67, No. 1, 2006, pp.311-336
Published online, 23rd August, 2005
DOI: 10.3987/COM-05-S(T)32
Synthesis and 2α-Modification of 24-Phenylvitamin D3 Lactones: Effects on VDR Antagonistic Activity

Nozomi Saito, Toshihiro Matsunaga, Hiroshi Saito, Miyuki Anzai, Kazuya Takenouchi, Daishiro Miura, Seiichi Ishizuka, Hiroaki Takayama, and Atsushi Kittaka*

*Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Teikyo University, 1091-1 Suarashi, Sagamiko-machi, Tsukui-gun, Kanagawa 199-0195, Japan


Novel vitamin D receptor (VDR) antagonists, 1α-hydroxy-24-phenylvitamin D3-26,23-lactones were synthesized by Trost’s methodology. The biological evaluation revealed that both the binding affinity for VDR and antagonistic activity were affected by the orientation of the phenyl group on the lactone ring. The modification of the 2α-position of the 24-phenylvitamin D3 lactones improved the antagonistic activity up to 41 times higher than that of TEI-9647.