Synthesis of 2alpha-substituted-14-epi-previtamin D3 and its genomic activity
Daisuke Sawada1, Tomoyuki Katayama, Yuya Tsukuda
1Faculty of Pharmaceutical Sciences, Teikyo University, Sagamiko, Kanagawa 229-0195, Japan.
Bioorganic & Medicinal Chemistry Letters
|August 21, 2009
Abstract:
We synthesized and isolated 2 alpha-substituted analogs of 14-epi-previtamin D3 after thermal isomerization at 80 degrees C for the first time. The VDR binding affinity and transactivation activity of osteocalcin promoter in HOS cells were evaluated, and the 2 alpha-methyl-substituted analog was found to have greater genomic activity than 14-epi-previtamin D3.
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