Synthesis of a compound libraries inspired by privileged structures of natural products
| Project/Area Number |
16310150
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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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 | Tohoku University (2005-2007)
Nagoya University (2004) |
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Principal Investigator |
ARIMOTO Hirokazu Tohoku University, Tohoku University, Graduate School of Life Sciences, Professor (60262789)
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| Project Period (FY) |
2004 – 2007
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| Project Status |
Completed (Fiscal Year 2007)
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| Budget Amount *help |
¥16,480,000 (Direct Cost: ¥15,400,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2007: ¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2006: ¥2,700,000 (Direct Cost: ¥2,700,000)
Fiscal Year 2005: ¥5,000,000 (Direct Cost: ¥5,000,000)
Fiscal Year 2004: ¥4,100,000 (Direct Cost: ¥4,100,000)
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| Keywords | biological activity / endogenous compound / library / 天然物 / 全合成 / オキサゾール / Beckmannn転位 / セオブロキシド / エリナシン / ケンドマイシン |
|---|
| Research Abstract |
Natural product is a rich source of bioactive substances. In this research project, I focused on the preparation of a compound library based on important partial structures (the privileged structures) involved in natural products.
At first I established the simple and efficient synthetic route to a plant growth regulator, theobroxide and its derivatives. Synthesis of a cytosolic phospholipase A2 inhibitor, pinnaic acid. Has also been established. Studies toward an antibiotic kendomycin, a cytotoxic material nakiterpiosin, aκ-opicid acceptor agonist, erinacine E were investigated, and their progress have been published as preliminary reports.
In the course of the research for identification of novel endogenous bioactive low molecular-weight compounds, Prof. Akaike group at Kumamoto University and I have reported an existence of 8-nitro-cGMP in various cell lines. Preliminary studies suggested that the molecule should play an important roles at the time of infection and inflammation in our bodies. The design and synthesis of chemical probe molecule are underway.
Furthermore, molecular shape of huge marine natural product, palytoxin, was elucidated by the synchrotron X-rays small angle scattering technique (SAXS). Direct observation of molecular shapes in solutions was accomplished with natural products for the first time. Palytoxin was proved to forms an associate dimer. Palytoxin have been shown to act on Na/K ATPase, and relationship of the associative nature with its biological activities should be an interesting future problem. Synthetic of a palytoxin-based library has investigated in this context.
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Report
(5 results)
Research Products
(25 results)
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[Journal Article] Protein S- guanylation by the biological signal 8-nitroguanosine 3',5'-cyclicmonophosphate2007
Author(s)
T. Sawa, M. H. Zaki, T. Okamoto, T. Akuta, Y. Tokutomi, S. K. Mitsuyama, H. Ihara, A. Kobayashi, M. Yamamoto, S. Fujii, H. Arimoto, T. Akaike
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Journal Title
Nature Chemical Biology 3
Pages: 727-735
NAID
Description
「研究成果報告書概要(和文)」より
Related Report
Peer Reviewed
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[Journal Article] Protein S- guanylation by the biological signal 8-nitroguanosine 3'',5''-cyclic monophosphate2007
Author(s)
Sawa, T.; Zaki, M. H.; Okamoto, T.; Akuta, T.;Tokutomi, Y.; Mitsuyama, S. K.-; lhara, H.; Kobayashi, A.; Yamamoto, M.; Fujii, S.; Arimoto, H.; Akaike T
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Journal Title
Nat Chem. Biol 3
Pages: 727-735
NAID
Description
「研究成果報告書概要(欧文)」より
Related Report
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[Journal Article] Protein S-guanylation by the biological signal 8-nitroguanosine 3',5'-cyclic monophosphate2007
Author(s)
T. Sawa, M. H. Zaki, T. Okamoto, T. Akuta, Y. Tokutomi, S. K. Mitsuyama, H. Ihara, A. Kobayashi, M. Yamamoto, S. Fujii, H. Arimoto, T. Akaike
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Journal Title
Nature Chemical Biology 3
Pages: 727-735
NAID
Related Report
Peer Reviewed
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