Synthesis of 2α-substituted-14-epi-previtamin D3 and its genomic activity

We synthesized and isolated 2α-substituted analogs of 14-epi-previtamin D3 after thermal isomerization at 80 °C for the first time. The VDR binding affinity and transactivation activity of osteocalcin promoter in HOS cells were evaluated, and the 2α-methyl-substituted analog was found to have greater genomic activity than 14-epi-previtamin D3.

2α-Substituted analogs of 14-epi-previtamin D3 showed greater genomic activity than 14-epi-previtamin D3 such as the VDR binding affinity and transactivation activity of osteocalcin promoter in HOS cells.Figure optionsDownload as PowerPoint slide