Synthesis and biological evaluation of hybrid acetogenins for the discovery of novel antitumor agents
| Project/Area Number |
21790113
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Drug development chemistry
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| Research Institution | Osaka University |
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Principal Investigator |
KOJIMA Naoto 大阪大学, 大学院・薬学研究科, 助教 (90420413)
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| Project Period (FY) |
2009 – 2010
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| Project Status |
Completed (Fiscal Year 2010)
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| Budget Amount *help |
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2010: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Fiscal Year 2009: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | 抗がん剤開発 / 構造活性相関 / 有機合成化学 / 抗腫瘍活性物質 / 生理活性 / 生理活性物質 |
|---|
| Research Abstract |
A series of α,β-unsaturated-γ-lactone-free nitrogen-containing heterocyclic analogues of solamin, a natural mono-THF acetogenin, have been synthesized and their cytotoxicity was investigated against 39 tumor cell lines. One of synthetic analogues, 1-methylpyrazol-5-yl derivative connected to THF moiety via an amide bond, exhibited approximately 10000 times higher cytotoxicity against HCT116, human colon cancer, than natural solamin.
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Report
(3 results)
Research Products
(60 results)
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[Journal Article] Convergent Synthesis of Fluorescence-Labeled Probes of Annonaceous Acetogenins and Visualization of Their Cell Distribution2010
Author(s)
Naoto Kojima, Takekuni Morioka, Daisuke Urabe, Masahiro Yano, Yuki Suga, Naoyoshi Maezaki, Ayako Ohhashi-Kobayashi, Yasuyuki Fujimoto, Masatomo Maeda, Takao Yamori, Takehiko Yoshimitsu, Tetsuaki Tanaka
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Journal Title
Bioorg. Med. Chem.
Volume: 18
Pages: 8630-8641
Related Report
Peer Reviewed
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