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 ,
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.
