APPROACH TO FUNCTION ELUCIDATION AND APPLICATION STUDY OF THE BIOACTIVE SUBSTANCES BY ORGANIC SYNTHESIS

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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.