| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2013: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2012: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2011: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
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| Research Abstract |
Based on our developed total synthesis of BKA, we conducted the structure-activity relationship study, which revealed three carboxylic acid groups of BKA plays an important role in staurosporin-induced apoptosis inhibitory activity of HeLa cells. Next, we designed and synthesized simpler derivatives and the conformation-restricted derivatives and then found that these derivatives showed potent apoptosis inhibitory activity. Consequently, we successfully achieved the design and synthesis in more easily available potent novel apoptosis inhibitors, which would be useful for highly sensitive fluorescent probes. The efficient asymmetric synthesis of xanthatin based on the highly stereoselective conjugate allylation of the -butenolide was also achieved.
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