| Budget Amount *help |
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2013: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2012: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
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| Research Abstract |
A cytotoxic peptide yaku'amide A was isolated from a marine sponge as an extremely potent cytotoxin. The growth-inhibitory activity of yaku'amide A against a panel of 39 human cancer cell lines is quite unique among known anticancer drugs. Therefore, it is suggested that yaku'amide A possesses new mode of action to exert its bioactivity. In order to evaluate its detailed biological activity, chemical synthesis for supplying material was required.
In this project, the development of a new assembly method of the dehydroamino acid residue utilizing Cu-mediated cross coupling reaction and the first total synthesis of yaku'amide A were achieved. In addition to this, another approach for the synthesis of Z-dehydroamino acid using Staudinger ligation was also established.
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