Search for new antitumor lead-compounds originated from plant alkaloids
| Project/Area Number |
22510224
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Living organism molecular science
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| Research Institution | Chiba University |
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Principal Investigator |
KITAJIMA Mariko 千葉大学, 大学院・薬学研究院, 准教授 (60195261)
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| Project Period (FY) |
2010 – 2012
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| Project Status |
Completed (Fiscal Year 2012)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2012: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2011: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2010: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
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| Keywords | 天然物化学 / 生物活性物質 / アルカロイド / インドール / コルヒチン / 誘導体合成 / プロドラッグ / 構造活性相関 / 細胞毒性 / 構造解析 |
|---|
| Research Abstract |
To discover and develop lead-compounds for new antitumor medicines originated from plant alkaloids, chemical investigation and biological evaluation of Gelsemium alkaloids and colchicinoids were carried out. As results, several novel alkaloids were isolated from Gelsemium plants. Key intermediates of sarpagine-type alkaloids, one of the members of Gelsemium alkaloids, were synthesized utilizing gold-catalyzed cyclization. 4-Halocolchicines and 4-chlorocolchicine derivatives bearing anα-hydroxyacetoamide side chain at C-7 were found to show potent antitumor activities. Pro-drugs of highly-active colchicine derivatives were prepared and their selective toxicity to the tumor cells was evaluated.
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Report
(4 results)
Research Products
(56 results)
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[Journal Article] Synthesis and Biological Evaluation of 4-Chlorocolchicine Derivatives as Potent Anticancer Agents with Broad Effective Dosage Ranges2012
Author(s)
H. Nishiyama, M. Ono, T. Sugimoto, T.Sasai, N. Asakawa, T. Matsumoto, T. Yaegashi, M. Nagaoka, T. Matsuzaki, N. Kogure, M. Kitajima, and H. Takayama
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Journal Title
Med. Chem. Comm
Volume: 3(12)
Issue: 12
Pages: 1500-1504
DOI
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Peer Reviewed
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[Presentation] New Monoterpenoid Indole Alkaloids from Gelsemium elegans2011
Author(s)
N. Kogure, Y. Yamada, M. Kitajima, S.Wongseripipatana and H. Takayama
Organizer
The 6^<th> International Conference on Cutting-Edge Organic Chemistry in Asia and 2^<nd> New Phase International Conference on Cutting-Edge Organic Chemistry in Asia (ICCEOCA-6/NICCEOCA-2)
Place of Presentation
HongKong, China
Year and Date
2011-12-12
Related Report
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[Presentation] ゲルセミ2010
Author(s)
山田洋介,北島満里子,小暮紀行,小林宏美,石井直子,Sumphan Wongseripipatana,高山廣光
Organizer
第52回天然有
Place of Presentation
静岡
Year and Date
2010-10-01
Related Report
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