| Project/Area Number |
26860065
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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 |
Natural medicines
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| Research Institution | Nagoya Institute of Technology (2015)
Osaka University (2014) |
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Principal Investigator |
Sumii Yuji 名古屋工業大学, 工学(系)研究科(研究院), 助教 (10612848)
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| Project Period (FY) |
2014-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2015: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2014: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Keywords | 海洋天然物 / 全合成 / 構造活性相関 / アナログ合成 / 細胞増殖抑制物質 / 抗結核物質 / ケミカルバイオロジー / 天然物 / ケミカルバイオジー |
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| Outline of Final Research Achievements |
We developed enantioselective synthesis of (+)-dictyoceratin-A and -C, hypoxia-selective growth inhibitors, from marine sponge. We tested the in vitro bioactivity of both enantiomers, and found that both enantiomers showed same hypoxia-selective growth inhibitory activity. We evaluated in vivo anti-tumor activity and structure-activity relationships of analogues of dictyoceratin-A and -C. We found that the whole structure of 1 or 2 is important for the hypoxia-selective growth inhibitory activity. We also synthesized bioactive probe molecular based on 1 and 2.
We succeeded the total synthesis of 3-alkylamino demethyl(oxy)aaptamine (3), an anti-dormant mycobacterial substance from marine sponge. We confirm the in vitro anti-dormant mycobacterial activity of 3. We also improved the synthetic methodology of 3 and successfully prepared hundreds milligram of 3. Moreover, we synthesized some analogues of 3 and found important information of structure-activity relationships.
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