2014 Fiscal Year Final Research Report
Exploration of the pharmacophore of antitumor peptide RA-VII that interacts with actin
| Project/Area Number |
24590024
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Chemical pharmacy
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| Research Institution | Tokyo University of Pharmacy and Life Science |
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Principal Investigator |
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| Project Period (FY) |
2012-04-01 – 2015-03-31
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| Keywords | 抗腫瘍活性 / RA-VII / アクチン / 環状ペプチド / アナログデザイン / ペプチド合成 / 細胞毒性 / 配座解析 |
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| Outline of Final Research Achievements |
Aza-cycloisodityrosine-, conformationally constrained side chain-bridged-, and fluorinated cycloisodityrosine analogues of RA-VII, a Rubia plant-origin antitumor cyclic peptide, were synthesized to improve the water solubility and explore the pharmacophore of RA-VII. The results indicated that the orientation of the aromatic rings of the cycloisodityrosine moiety is important to express the cytotoxic activity and increase of the electron density of those aromatic rings decreases the activity. A new dimeric RA-series peptide was isolated from R. cordifolia, whose structure gave us some information about the biosynthesis of this series of peptides. In addition, sixteen new compounds were isolated from Stemona tuberosa and Eurycoma longifolia to develop chemical library for the screening assay.
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| Free Research Field |
天然物化学
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