Synthesis of novel 1α,25-dihydroxy-19-norvitamin D3 with an amide conjugate

Yoshitomo Suhara, Keiichiro Ono, Akihiro Yoshida, Toshie Fujishima, Nozomi Saito, Shinobu Honzawa, Seishi Kishimoto, Takayuki Sugiura, Keizo Waku, Hiroaki Takayama, Atsushi Kittaka

研究成果: Article査読

4 被引用数 (Scopus)

抄録

The diene system of 1α,25-dihydroxy-19-norvitamin D3 was replaced by a stable amide bond. A 3-hydroxypropoxy group, which was effective on enhancing binding affinity of 1α,25-dihydroxyvitamin D3 for vitamin D receptor (VDR), was introduced to the C2-position of the amide type analogue of 1α,25-dihydroxy-19-norvitamin D3. The amide analogue was found to be not suitable for binding to the ligand binding domain of the bovine thymus VDR, and additional modification at the C2-position did not improve the affinity. Potency in induction of HL-60 cell differentiation was evaluated for the novel amide analogues (3a-c).

本文言語English
ページ(範囲)423-436
ページ数14
ジャーナルHeterocycles
62
DOI
出版ステータスPublished - 2004 1月 1
外部発表はい

ASJC Scopus subject areas

  • 分析化学
  • 薬理学
  • 有機化学

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