Bioactive compounds utilizing interactions between cell membrane and membrane proteins

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Practical total synthesis of bongkrekic acid(BKA) was achieved via our convergent strategy, and more than 10 mg of BKA was obtained. Based on these results, the BKA derivatives were also synthesized. We also established an assay protocol for staurosporin-induced apoptosis inhibitory activity of the HeLa cells. For apoptosis inhibitory activity, three carboxylic acid groups of BKA were found to be important. The analogues having only two carboxylates showed cell toxicity. The phospholipid-containing dicarboxylic acid analogues had an inhibitory activity of apoptosis. These results would give a clue for development of more efficient and easily available novel apoptosis inhibitors.