| Project/Area Number |
22659023
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Single-year Grants |
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| Research Field |
Drug development chemistry
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| Research Institution | Kyushu University |
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Principal Investigator |
SHINDO Mitsuru 九州大学, 先導物質化学研究所, 教授 (40226345)
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| Co-Investigator(Renkei-kenkyūsha) |
SHINOHARA Yasuo 徳島大学, 疾患ゲノム研究センター, 教授 (60226157)
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| Project Period (FY) |
2010 – 2011
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| Project Status |
Completed (Fiscal Year 2011)
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| Budget Amount *help |
¥3,090,000 (Direct Cost: ¥2,700,000、Indirect Cost: ¥390,000)
Fiscal Year 2011: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2010: ¥1,400,000 (Direct Cost: ¥1,400,000)
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| Keywords | 生物活性物質 / アポトーシス / 生物機能性分子 / 阻害剤 / ボンクレキン酸 / 有機合成化学 / 膜たんぱく質 / 構造活性相関 / 天然有機化合物 / 膜タンパク質 |
|---|
| Research Abstract |
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.
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