Structure-activity relationship study of hybrid acetogenins toward the practical use
Project/Area Number |
23790130
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Research Category |
Grant-in-Aid for Young Scientists (B)
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Allocation Type | Multi-year Fund |
Research Field |
Drug development chemistry
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Research Institution | Kyoto Pharmaceutical University (2012-2013) Osaka University (2011) |
Principal Investigator |
KOJIMA Naoto 京都薬科大学, 薬学部, 講師 (90420413)
|
Project Period (FY) |
2011 – 2012
|
Project Status |
Completed (Fiscal Year 2013)
|
Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2012: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
Fiscal Year 2011: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
|
Keywords | 抗がん剤 / 有機合成化学 / 生物活性物質 / 構造活性相関 / 構造活性相関研究 / 抗腫瘍活性物質 / 生物活性 |
Research Abstract |
We planed the exploring mode of action of hybrid acetogenins that we recently found novel lead compounds for anticancer agents. The convergent synthesis of fluorescence-labeled hybrid acetogenin was accomplished by two asymmetric alkynylations of 2,5-diformyl tetrahydrofuran with an alkyne tagged with fluorescent groups and another alkyne with thiophen ring. The merged fluorescence of labeled hybrid acetogenin and MitoTracker Red suggests that hybrid acetogenins localize in the mitochondria. The derivative with terminal amino group was also synthesized for affinity column chromatography.
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Report
(4 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
Issue: 19
Pages: 3841-3846
DOI
Related Report
Peer Reviewed
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小島直人,伏見哲也,立川貴啓,戸田雄也,大槻一文,好光健彦,田中徹明,岡村睦美,矢守隆夫,岩﨑宏樹,山下正行
Organizer
日本薬学会第133年会
Place of Presentation
パシフィコ横浜(神奈川)
Year and Date
2013-03-28
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[Presentation] チオフェン環を導入したアセトゲニン類アナログの合成と抗腫瘍活性評価2012
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大槻一文,小島直人,伏見哲也,立川貴啓,戸田雄也,好光健彦,田中徹明,岡村睦美,矢守隆夫,岩﨑宏樹,山下正行
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第32回有機合成若手セミナー
Place of Presentation
神戸薬科大学(兵庫)
Year and Date
2012-11-22
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[Presentation] ハイブリッド型アセトゲニン類の合成と抗腫瘍活性評価2012
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小島直人,大槻一文,伏見哲也,立川貴啓,戸田雄也,好光健彦,田中徹明,岡村睦実,矢守隆夫,岩﨑宏樹,山下正行
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第19回天然薬物の開発と応用シンポジウム
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Year and Date
2012-11-02
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第62回日本薬学会近畿支部大会
Place of Presentation
武庫川女子大学(兵庫)
Year and Date
2012-10-20
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[Presentation] ハイブリッド型アセトゲニン類の複素環部位の変換と抗腫瘍活性評価2012
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小島直人,大槻一文,伏見哲也,立川貴啓,戸田雄也,好光健彦,田中徹明,岡村睦実,矢守隆夫,岩﨑宏樹,山下正行
Organizer
第62回日本薬学会近畿支部大会
Place of Presentation
武庫川女子大学(兵庫)
Year and Date
2012-10-20
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[Presentation] 蛍光標識化アセトゲニン類の収束的合成法の開発とその細胞内動態2011
Author(s)
須賀友規,小島直人,森岡建州,矢野昌弘,浦辺大輔,前﨑直容,大橋綾子,藤本康之,前田正知,矢守隆夫,田中徹明
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第31回有機合成若手セミナー
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京都大学(京都)
Year and Date
2011-11-16
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[Presentation] 蛍光標識化アセトゲニン類の収束的合成法の開発とその細胞内動態2011
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小島直人,須賀友規,森岡建州,矢野昌弘,浦辺大輔,前﨑直容,大橋綾子,藤本康之,前田正知,矢守隆夫,田中徹明
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第61回日本薬学会近畿支部大会
Place of Presentation
神戸学院大学(兵庫)
Year and Date
2011-10-22
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