2011 Fiscal Year Final Research Report
Structure-activity relationship study of hatermalides by using medicinal chemistry
| Project/Area Number |
21510221
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Living organism molecular science
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| Research Institution | University of Tsukuba |
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Principal Investigator |
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| Project Period (FY) |
2009 – 2011
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| Keywords | 天然物有機化学 / 有機合成化学 / 腫瘍細胞増殖阻害 / 構造活性相関 |
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| Research Abstract |
Haterumalides and biselides are cytotoxic macrolide isolated from the Okinawan marine animals. Interestingly, haterumalide NA showed strong toxicity against brine shrimp, while haterumalide NA methyl ester and biselide A are less toxic. I planned to synthesize haterumalide derivatives and to evaluate its biological activity. As a result, I elucidated that chloroolefin part of haterumalides is essential for the strong cytotoxicity of haterumalides. Also, I have achieved the synthesis of core carbon framework of biselide E.
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