Structure activity relationship study of bile acid derivatives to development of novel vitamin D receptor ligand
| Project/Area Number |
15K08018
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Tokyo Medical and Dental University |
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Principal Investigator |
MASUNO Hiroyuki 東京医科歯科大学, 生体材料工学研究所, 技術専門職員 (80376714)
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| Project Period (FY) |
2015-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2017: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2016: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Keywords | ビタミンＤ / 核内受容体 / 胆汁酸 / 構造活性相関 / ビタミンD |
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| Outline of Final Research Achievements |
To develop potent vitamin D receptor ligand which have no vitamin D skeleton and to investigate structure and activity relationships of lithocolic acid derivateves, I designed, synthesized and evaluated biological activity of novel lithocholic acid derivateves. I synthesized several lithocholic acid derivatives which have hydoxyl group containing alkyl group at carbon three on steroid skeleton. The vitamin D receptor activity of synthesized compounds were evaluated by differentiation-inducing activity in HL-60 human promyelocytic leukemia cell line. All of the compounds have higher activity than known lithocholic acid derivatives. The most potent compound have activity as well as 1,25-dihydroxyvitamin D3. These compounds have enough activities to use clinical application.
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Report
(4 results)
Research Products
(5 results)
