海洋起源抗腫瘍活性環状ペプチドの合成研究
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概要
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Cyclic peptides from marine organisms constitute a growing class of naturally occurring cytotoxic substances. A general synthetic method for thiazole amino acids, common components of these cyclic peptides 1-7,has been developed and total syntheses of 1-7 have been achieved. In the process, dolastatin 3 (1) with the proposed structure has been disclosed to differ from the natural material and the real structure 2 has been confirmed by its total synthesis. Patellamides (5) with the proposed structures have been revised to be 6 by their total syntheses. Absolute configuration of ascidiacyclamide (4) has been determined to be 4 and the structure of ulithiacyclamide (7) has been confirmed. Ulicyclamide (3) has been efficiently prepared in combination with solid and liquid phase syntheses. Didemnins A and B (9a and 9b), cyclic depsipeptides with potent antitumor activity, have been prepared by condensation of the key eastern and western fragments.
- 公益社団法人日本薬学会の論文
- 1991-01-25