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Synthesis of 2α-substituted-14-epi-previtamin D3 and its genomic activity |
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| Authors: | Daisuke Sawada Tomoyuki Katayama Yuya Tsukuda Nozomi Saito Masashi Takano Hiroshi Saito Ken-ichiro Takagi Eiji Ochiai Seiichi Ishizuka Kazuya Takenouchi Atsushi Kittaka |
| Affiliation: | aFaculty of Pharmaceutical Sciences, Teikyo University, Sagamiko, Kanagawa 229-0195, Japan;bTeijin Institute for Bio-medical Research, Teijin Pharma Ltd., Tokyo 191-8512, Japan |
| Abstract: | 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. |
| Keywords: | Vitamin D3 14-Epi-previtamin D3 Osteocalcin Vitamin D receptor |
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