Structure activity relationships study of dual-core type acetogenin analogues for development of novel antitumor agents
| Project/Area Number |
25460159
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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 | Kyoto Pharmaceutical University |
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Principal Investigator |
Kojima Naoto 京都薬科大学, 薬学部, 准教授 (90420413)
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| Co-Investigator(Kenkyū-buntansha) |
山下 正行 京都薬科大学, 薬学部, 教授 (20239982)
岩崎 宏樹 京都薬科大学, 薬学部, 助教 (70582592)
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| Project Period (FY) |
2013-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2014: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2013: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Keywords | 抗がん剤 / 有機合成化学 / 構造活性相関研究 / 生物活性物質 / 構造活性相関 |
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| Outline of Final Research Achievements |
We reported that heterocycle-introduced analogues in the place of lactone ring as a common structure of annonaceous acetogenins, potently inhibit the growth of human cancer cell lines. Especially, a thiophen analog showed potent antitumor activity in in vivo assay using xenograft mice. In this work, we planned to synthesis of dual-core type analogues those have two heterocycles at the both ends of those. As a result, it was revealed that dual-core type analogue shows as potent inhibitory activity as the mother compound, indicating that dual-core type analogues may be a novel lead compound for antitumor agents.
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Report
(5 results)
Research Products
(71 results)
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[Journal Article] First asymmetric total synthesis of (+)-taiwaniaquinol D and (?)-taiwaniaquinone D by using intramolecular Heck reaction2013
Author(s)
Minoru Ozeki, Megumi Satake, Toshinori Toizume, Shintaro Fukutome, Kenji Arimitsu, Shinzo Hosoi, Tetsuya Kajimoto, Hiroki Iwasaki, Naoto Kojima, Manabu Node, Masayuki Yamashita
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Journal Title
Tetrahedron
Volume: 69
Pages: 3841-3846
DOI
Related Report
Peer Reviewed
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