Design, synthesis and biological evaluation of novel 1α,25-dihydroxyvitamin D3 analogues possessing aromatic ring on 2α-position

In the present study, we describe the synthesis of new analogues of 1α,25-dihydroxyvitamin D 3 ( 1 ), 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.