| Budget Amount *help |
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2015: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2014: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2013: ¥3,120,000 (Direct Cost: ¥2,400,000、Indirect Cost: ¥720,000)
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| Outline of Final Research Achievements |
The peptides contained with unusual amino acids show several biological activities, especially anti-HIV activity. We have attempted to synthesize cyclic depsipeptides callipeltins and homopymines with several unusual amino acids. Preparation of unusual amino acids were achieved by stereoselective synthesis in solution phase. Peptide constructions were used by standard Fmoc-solid phase peptide synthesis and cyclization and final deprotection were proceeded smoothly by optimized conditions to give callipeltin B and cyclic fragment of homophymines. We found that purified callipeltin B included the contamination of callipeltins C and H at a ratio of approximately 15%. These results suggested that the cytotoxicity of natural callipeltin B was derived from callipeltins C and H. On the other hand, TAK779 bound with coumarin was attempted for the preparation of new method of evaluation of anti-HIV activities.
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