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

Research output: Contribution to journalArticle

7 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)1431-1433
Number of pages3
JournalChemical and Pharmaceutical Bulletin
Volume57
Issue number12
DOIs
Publication statusPublished - Dec 1 2009
Externally publishedYes

Keywords

  • C4-modified seco-steroid
  • Osteocalcin
  • Previtamin D
  • Vitamin D
  • Vitamin D receptor

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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  • Cite this

    Sawada, D., Tsukuda, Y., Saito, H., Takagi, K. I., Horie, K., Ochiai, E., Takenouchi, K., & Kittaka, A. (2009). Synthesis and biological evaluation of 4-substituted vitamin D and 14-epi-previtamin D analogs. Chemical and Pharmaceutical Bulletin, 57(12), 1431-1433. https://doi.org/10.1248/cpb.57.1431