Synthesis and evaluation of A-ring diastereomers of 1α,25-dihydroxy-22-oxavitamin D3 (OCT)

Susumi Hatakeyama, Toshio Okano, Junji Maeyama, Tomoyuki Esumi, Hiroko Hiyamizu, Yoshiharu Iwabuchi, Kimie Nakagawa, Keiichi Ozono, Akira Kawase, Noboru Kubodera

研究成果: Article査読

13 被引用数 (Scopus)

抄録

A-ring diastereomers of 1α,25-dihydroxy-22-oxavitamin D3 (OCT) (2), 3-epi-1α,25-dihydroxy-22-oxavitamin D3 (3-epiOCT) (3) and 1,3-diepi-1α,25-dihydroxy-22-oxavitamin D3 (1,3-diepiOCT) (4) were synthesized by the convergent method. In vitro binding affinity for rat vitamin D binding protein and calf-thymus vitamin D receptor, differentiation-inducing activity on HL-60 cells, and transcriptional activity of 3-epiOCT (3) and 1,3-diepiOCT (4) were evaluated in comparison with OCT (2), 1-epi-1α,25-dihydroxy-22-oxavitamin D3 (1-epiOCT) (5) and 1α,25-dihydroxyvitamin D3 (1).

本文言語English
ページ(範囲)403-415
ページ数13
ジャーナルBioorganic and Medicinal Chemistry
9
2
DOI
出版ステータスPublished - 2001
外部発表はい

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

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