海洋环肽Phakellistatin 13的全合成研究

Phakellistatin 13是从海绵中分离得到的高活性的抗肿瘤环七肽化合物, 是优良的抗肿瘤先导化合物. 我们结合逐步接肽法和片段缩合法, 首次采用液相法完成Phakellistatin 13的全合成, 并提出与以往报道不同的多肽环合策略. 目标化合物经质谱与核磁共振光谱结构确证与天然产物一致, 为进一步开展Phakellistatin 13及其类似物的抗肿瘤活性研究打下了扎实的基础.

Total Synthesis of A Marine Cyclopeptide: Phakellistatin 13

Phakellistatin 13 is a cycloheptapeptide isolated from sponge and show good suppression action to human hepatoma BEL-7404 cell line. We synthesized Phakellistatin 13 the first time by solution method combination of stepwise coupling and segment condensation and the final deprotection and cyclization were achieved according to our designed method, which was different from the reported process. Comparison of the natural and synthetic specimens of phakellistatin 13 by 1H and 13C NMR spectra gave identical NMR signals. The total synthesis of phakellistatin 13 is significant to further study its derivatives and develop novel antitumor drugs.