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Synthetic Studies on Optically Active Substances with Remarkable Bioactivities to Analyze Their Biological Functions

具有显着生物活性的光学活性物质的合成研究及其生物学功能

基本信息

批准号：
09460056
负责人：
KITAHARA Takeshi
金额：
$ 7.74万
依托单位：
The University of Tokyo
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (B)
财政年份：
1997
资助国家：
日本
起止时间：
1997 至 1998
项目状态：
已结题

项目摘要

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.

1.研究了具有较强细胞增殖抑制活性的根赤霉素、乙酰苯酞和普鲁辛的合成。我们不仅可以完成天然产物的合成，还可以完成相关类似物的合成，包括生物素衍生物。结果表明，乙酰酞苷的部分类似物具有相似的活性，普鲁辛的8种可能的立体异构体也具有相似的活性.合成了植物生长调节剂，如茉莉素，pironetin，specifernin，sorokinianin等，并进行了SAR研究。其中吡柔酮是一种生物素化的类似物，可选择性地与微管结合，目前正在进行功能分析研究.与植物保护和植物营养相关的天然产物及其类似物的合成。例如，昆虫拒食剂是一种很有前途的生态耐受农药。我们成功地合成了印楝素B环骨架和另一种拒食剂tanabalin。这些方法将被应用于合成相关分子，以研究其生物活性。发展了植物铁载体的快速合成方法，并进行了类似物的合成，以创造更简单但更好的衍生物.完成了吡咯烷和哌啶类似物的合成，如坏死霉素、DAB-1、LAB-1、野尻霉素及其具有有效葡萄糖苷酶抑制剂的类似物。