2014 Fiscal Year Final Research Report
Syntheses of novel ligands that maintain these unique biological activities in vivo
| Project/Area Number |
25860011
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Chemical pharmacy
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| Research Institution | Teikyo University |
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Principal Investigator |
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| Project Period (FY) |
2013-04-01 – 2015-03-31
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| Keywords | ビタミンD / 合成化学 / 生理活性 / 有機化学 / 薬学 |
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| Outline of Final Research Achievements |
The synthesis of 1α,2α,25-trihydroxyvitamin D3, which is the major metabolite of 2α-(3-hydroxypropoxy)-1α,25-dihydroxyvitamin D3 (O2C3) by CYP3A4, has been achieved. Convergent syntheses of several novel 19-norvitamin D analogs with a tetrazole ring at the C2 position possessing the propyl linker have been achieved. These syntheses are characterized as useful syntheses with the high efficiency and yield, so that other ligands would be synthesized in these synthetic ways. Binding affinity for vitamin D receptor (VDR) of these ligands, transactivation activity of osteocalcin promoter in HOS cells, and metabolism by CYP24A1 have been also studied.
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| Free Research Field |
有機合成化学
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