2017 Fiscal Year Final Research Report
Medicinal chemistry study of bioactive marine natural products targeting tumor microenvironment
| Project/Area Number |
15K07996
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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 |
Natural medicines
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| Research Institution | Ritsumeikan University (2017)
Osaka University (2015-2016) |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
ARAI MASAYOSHI 大阪大学, 薬学研究科, 特任教授 (80311231)
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| Project Period (FY) |
2015-04-01 – 2018-03-31
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| Keywords | 天然活性物質 / 海洋天然物 / 創薬化学 / 抗がん剤 / がん微小環境 |
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| Outline of Final Research Achievements |
Medicinal chemistry study of bioactive marine natural products targeting tumor microenvironment were executed. As for biakamides, novel polyketides as selective growth inhibitors against cancer cells under glucose-deprived condition, total synthesis and structure-activity relationship study were accomplished. Then, mechanistic study of biakamides using photoaffinity probe revealed that biakamides inhibited the respiratory complex I in mitochondria.
We also analyzed the structure-activity relationship of furospinosulin-1, hypoxia-selective growth inhibitor against cancer cells, for developing potent anti-cancer drug leads, and revealed that structural modification at the end of side chain by PEG and some polar substituents were effective to improve cell permeability and growth inhibitory activity toward cancer cells.
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| Free Research Field |
天然物有機化学
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