Abstract
2β-Substituted analogs of 14-epi-previtamin D 3 were synthesized for the first time by the thermal isomerization of the corresponding 14-epi-vitamin D 3 that were available using coupling reaction between the A-ring phosphine oxide derived from a chiral epoxide and CD-ring cis-hydrindanone. The VDR binding affinity and transactivation activity of osteocalcin promoter in HOS cells were evaluated, and the new analogs were found to be less active, 0.01–0.18% of VDR binding affinity compared with the natural hormone and EC 50 1.0–9.1 nM for transactivation activity, than 14-epi-previtamin D 3 with 0.5% (VDR) and EC 50 0.46 nM, respectively.
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