| Budget Amount *help |
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2014: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2013: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2012: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
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| Outline of Final Research Achievements |
Facile synthetic approaches to peptide natural products with multiple N-methyl amide bonds were investigated. For the synthesis of antiproliferative coibamide A, the solid-phase protocols were optimized. The macrolactonization of the linear precursor provided a coibamide A epimer with slightly less potent antiproliferative activity. Additionally, a facile synthetic process of IB-01212 via multiple N-methylation was established. The structure-activity relationship of a series of the derivatives revealed that the peptide conformation would mainly contribute to the bioactivity.
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