| Project/Area Number |
09460056
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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 |
Bioproduction chemistry/Bioorganic chemistry
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| Research Institution | The University of Tokyo |
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Principal Investigator |
KITAHARA Takeshi The University of Tokyo, Graduate School of Agricultural and life Sciences, Professor, 大学院・農学生命科学研究科, 教授 (40087573)
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| Co-Investigator(Kenkyū-buntansha) |
WATANABE Hidenori The University of Tokyo, Graduate School of Agricultural and life Sciences, Asso, 大学院・農学生命科学研究科, 助教授 (00202416)
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| Project Period (FY) |
1997 – 1998
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| Project Status |
Completed (Fiscal Year 1998)
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| Budget Amount *help |
¥12,100,000 (Direct Cost: ¥12,100,000)
Fiscal Year 1998: ¥2,600,000 (Direct Cost: ¥2,600,000)
Fiscal Year 1997: ¥9,500,000 (Direct Cost: ¥9,500,000)
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| Keywords | Bioactive molecules / Optically active substances / Structure-Activity-Relation / Inhibitor of cell progression / Insect antifeedant / Plant growth regulators / Biotinylated probes / Enzyme inhibitors / 植物成長調節剤 / ジャスモノイド / ラデシコール / アセトフタリデン / ネクトシリン / ソロキンアニン / 植物生長調節剤 |
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| Research Abstract |
1. Synthesis of radicicol, acetophthalidin and preussin, which show potent inhibition activities against cell-progression was studied. We could finish the synthesis not only of natural products but also related analogs including biotinylated derivatives. As a result, we found that some analogs of acetophthalidin have the similar activities and also all the possible 8 stereoisomers of preussin have the same activity at the similar level.
2. Synthesis of plant-growth regulators, such as jasmonoids, pironetin, specifernin, sorokinianin and so on was also accomplished and SAR studies were performed. In the case of pironetin, one of biotinylated analogs bound selectively with micro tubule and now the study on the analysis of function is underway.
3. Synthesis of natural products and analogs related to plant protection and plant nutrition. For example, insect antifeedant is a promising pesticide tolerant to eco-system. We succeeded in the synthesis of azadirachtin B-ring skeleton and also another antifeedant, tanabalin via very efficient scheme. These methodologies would be applied to synthesize related molecules to study their biological activities. Expeditious synthesis of phytosiderophores was developed and the synthesis of analogs was executed to create simpler but better derivatives.
4. Synthesis of pyrrolidine and piperidine analogs, such as nectrisine, DAB-1, LAB-1, nojirimycin and their analogs with potent glucosidase inhibitors was achieved.
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