Title of article
Spirocyclic piperidines; Pharmacophore model; Molecular modeling experiments; Theoretical considerations
Author/Authors
Shinobu Honzawa، نويسنده , , Yasuhiro Yamamoto، نويسنده , , Atsushi Yamashita، نويسنده , , Takayuki Sugiura، نويسنده , , Masaaki Kurihara، نويسنده , , Midori A. Arai، نويسنده , , Shigeaki Kato، نويسنده , , Atsushi Kittaka، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
23
From page
3002
To page
3024
Abstract
We designed and synthesized 1α- and 1β-hydroxymethyl-2α-(3-hydroxypropyl)-25-hydroxyvitamin D3 (2a,b) and related analogues 2α-(3-hydroxypropyl)-25-hydroxyvitamin D3 (3), Posner’s analogues of 1α- and 1β-hydroxymethyl-25-hydroxyvitamin D3 (4a,b), as well as 2α-(3-hydroxypropyl)-1α,25-dihydroxyvitamin D3 (5), to confirm the effect of the 1α-hydroxy group and/or 2α-(3-hydroxypropyl) group of vitamin D3 analogues with the modified A-ring moiety on the mutant vitamin D receptor, VDR(Arg274Leu). The 2α-(3-hydroxypropyl) group showed better effect on enhancement of the transcriptional activity through the mutant VDR than the 1α- and 1β-hydroxymethyl groups.
Keywords
Vitamin D receptor , Mutant vitamin D receptor , Structure–function relationships , Vitamin D analogues
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2008
Journal title
Bioorganic and Medicinal Chemistry
Record number
1304134
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