APPROACH TO FUNCTION ELUCIDATION AND APPLICATION STUDY OF THE BIOACTIVE SUBSTANCES BY ORGANIC SYNTHESIS
| Project/Area Number |
11660102
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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 |
Bioproduction chemistry/Bioorganic chemistry
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| Research Institution | THE UNIVERSITY OF TOKYO |
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Principal Investigator |
WATANABE Hidenori GRADUATE SCHOOL OF AGRICALTURAL AND LIFE SCIENCES, THE UNIVERSITY OF TOKYO, ASSOCIATE PROFESSOR, 大学院・農学生命科学研究科, 助教授 (00202416)
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| Project Period (FY) |
1999 – 2001
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| Project Status |
Completed (Fiscal Year 2001)
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| Budget Amount *help |
¥3,100,000 (Direct Cost: ¥3,100,000)
Fiscal Year 2001: ¥600,000 (Direct Cost: ¥600,000)
Fiscal Year 2000: ¥600,000 (Direct Cost: ¥600,000)
Fiscal Year 1999: ¥1,900,000 (Direct Cost: ¥1,900,000)
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| Keywords | FR901461 / KAITOCEPHALIN / CELL CYCLE INHIBITOR / NEUROPROTECTIVE SUBSTANCE / STEREOSELECTIVE SYNTHESIS / 類縁体合成 / 構造-活性相関 / アセトフタリジン / プリュッシン |
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| Research Abstract |
The total synthesis of FR9014614, a cell cycle inhibitor was accomplished from *-methyl intermediate, which possesses higher activity than the natural one. *-Biotinylated analog was also prepared from FR901464 and using this compound as a probe, isolation and identification of the binding protein and analysis of its function is in progress.
By the total synthesis of kaitocephalin, a neuroprotective substance, it was found that the stereostructure had been misassigned. Comparison of spectral data of several stereoisomers and simplified analogs with those of the natural compound suggested a correct stereostructure. The revised structure was confirmed by the total synthesis. Bioassay of the synthetic stereoisomers and analogs gave interesting informations about the structure-activity relationships.
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Report
(4 results)
Research Products
(17 results)
