2011 Fiscal Year Final Research Report
Bioactive compounds utilizing interactions between cell membrane and membrane proteins
| 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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| Keywords | 生物活性物質 |
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| 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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[Journal Article] Xanthatin selectively induces GADD45・and stimulates caspase-independent cell death in human breast cancer MDA-MB-231 cells, Takeda2011
Author(s)
S.; Matsuo, K.; Yaji, K.; Okajima-Miyazaki, S.; Harada, M.; Miyoshi, H.; Okamoto, Y.; Amamoto, T.; Shindo, M.; Omiecinski, C. J.; Aramaki, H.
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Journal Title
Chemical Research in Toxicology
Volume: 24
Pages: 855-865
Peer Reviewed
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