Synthetic Studies on Optically Active Substances Directed towards the Creation of Novel Functional Materials

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1) Syntheses of enzyme inhibitors and cell-cycle inhibitors were studied. Total syntheses of several inhibitors have been accomplished during these two years, for example, preussin, FR901464, pironetin, etc. Related analogs including biotinylated probes of radicicol, pironetin. FR901464 and preussin were synthesized and submitted to biological studies. In the case of FR901464, it was found that some analogs were much more biologically active than natural product and also target protein was identified. Further studies on the analysis of biological functions of these probes as well as related analogs are under investigation. In the case of pironetin, we found that this compound binds to tublin selectively and also did precise structure-activity relationship and found stereochemistry of side chain is rather important.2) Syntheses of substances related to plant protection and plant physiology are also studied and we developed the route to azadirachtin, a potent insect-antifeedant, by exploiting the radical cyclization method to create basic carbon skeleton. We are trying to apply this method to the real system. In the case of deoxymugineic acid (DMA) and analogs, we found very interesting results that some analogs are more active than DMA and we are now applying these substances for field test.Through two years, we accomplished to synthesize very interesting molecules with remarkable bioactivities and by collaborating with biologists, biochemists and physiologists, we are going to accumulate interesting biological data. We will continue these studies more.