2012 Fiscal Year Final Research Report
Design and synthesis of the inhibitors for chemokine receptor CCR5
| Project/Area Number |
21689004
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| Research Category |
Grant-in-Aid for Young Scientists (A)
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| Allocation Type | Single-year Grants |
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| Research Field |
Drug development chemistry
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| Research Institution | Yamagata University |
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Principal Investigator |
KONNO Hiroyuki 山形大学, 大学院・理工学研究科, 准教授 (50325247)
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| Project Period (FY) |
2009 – 2012
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| Keywords | 環状ペプチド / 抗 HIV活性 / ケモカインレセプター / 固相合成 / 異常アミノ酸 |
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| Research Abstract |
Callipeltins are linear-and cyclic depsi-peptides isolated from marine sponge by Zampella's group. These molecules were reported to exhibit anti-HIV activity and cytotoxicity against various tumor cell lines. In the course of our recent research regarding the synthetic study of cyclic depsipeptides, we conducted studies on the synthesis of callipeltins supposed to be efficient structures for CCR5 inhibitors as anti-HIV drugs or anti-cancer agents. In the present study, we performed the stereoselective synthesis of several unusual amino acids and solid phase synthesis of callipeltin E, M and B on Fmoc-strategy. In addition, we evaluated the cytotoxicity against the Hela cell line.
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