Synthesis and Biological Evaluation of 4-Substituted Vitamin D and 14-Epi-Previtamin D Analogs

Daisuke Sawada; Yuya Tsukuda; Hiroshi Saito; Ken-ichiro Takagi; Kyouhei Horie; Eiji Ochiai; Kazuya Takenouchi; Atsushi Kittaka

doi:10.1248/cpb.57.1431

Notes

Synthesis and Biological Evaluation of 4-Substituted Vitamin D and 14-Epi-Previtamin D Analogs

Daisuke Sawada, Yuya Tsukuda, Hiroshi Saito, Ken-ichiro Takagi, Kyouhei Horie, Eiji Ochiai, Kazuya Takenouchi, Atsushi Kittaka

Author information

Keywords: vitamin D₃, previtamin D₃, C4-modified seco-steroid, vitamin D receptor, osteocalcin

JOURNAL FREE ACCESS

2009 Volume 57 Issue 12 Pages 1431-1433

DOI https://doi.org/10.1248/cpb.57.1431

Details

Abstract

We synthesized the 4-hydroxy and 4-methoxy analogs of active vitamin D₃ (1α,25(OH)₂D₃, 1) and its C14-epimer with the previtamin D₃ form of 14-epi-1α,25(OH)₂preD₃ (14-epi-pre1). Their vitamin D receptor (VDR) binding affinity and osteocalcin promoter transactivation activity in HOS cells were evaluated, and had lower activity than the natural hormone (1) and 14-epi-pre1, respectively.

Corresponding author

Register with J-STAGE for free!