Title of article
Design, synthesis and biological evaluation of novel 1α,25-dihydroxyvitamin D3 analogues possessing aromatic ring on 2α-position
Author/Authors
Shinobu Honzawa، نويسنده , , Koshiro Hirasaka، نويسنده , , Yasuhiro Yamamoto، نويسنده , , Sara Peleg، نويسنده , , Toshie Fujishima، نويسنده , , Masaaki Kurihara، نويسنده , , Nozomi Saito، نويسنده , , Seishi Kishimoto، نويسنده , , Takayuki Sugiura، نويسنده , , Keizo Waku، نويسنده , , Hiroaki Takayama، نويسنده , , Atsushi Kittaka، نويسنده ,
Issue Information
هفته نامه با شماره پیاپی سال 2005
Pages
11
From page
11253
To page
11263
Abstract
In the present study, we describe the synthesis of new analogues of 1α,25-dihydroxyvitamin D3 (), which possess hydrophobic aromatic ring on the 2α position. Among these analogues, 2α-benzyl analogue showed the highest potency in the affinity for the wild type vitamin D receptor (VDR) and induction of HL-60 cell differentiation as well as transcriptional activity. Affinity for the mutant VDR related to hereditary vitamin D-resistant rickets (R274L) was also examined.
Keywords
Vitamin D receptor , Aromatic ring , Ligand binding domain
Journal title
Tetrahedron
Serial Year
2005
Journal title
Tetrahedron
Record number
1089351
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