PDF(Pubmed)
Abstract：
In our continuing search for biologically active new chemical entities from marine organisms, we have isolated a new cyclic depsipeptide, PM170453 (1), from a cyanobacterium of the genus Lyngbya sp., collected in the Indo-Pacific Ocean. Structure elucidation of the isolated compound was determined by spectroscopic methods including MS, 1H, 13C and 2D-NMR. To solve the supply problem for 1 and progress pharmaceutical development, the total synthesis of 1 that involves a total of 20 chemical steps in a convergent process was carried out. Its in vitro cytotoxic activity against four human tumor cell lines, as well as the inhibition of the interaction between the programmed cell death protein 1 PD-1 and its ligand PD-L1 were also evaluated.
摘要：
在我们不断从海洋生物中寻找具有生物活性的新化学实体的过程中，我们分离出一种新的环状缩肽,PM170453(1),来自Lyngbyasp属的蓝细菌。,收集在印度洋-太平洋。通过包括MS在内的光谱法确定分离化合物的结构阐明，1H,13C和2D-NMR。为解决1的供应问题和推进药物开发，进行1的总合成，该合成在会聚过程中涉及总共20个化学步骤。其对四种人类肿瘤细胞系的体外细胞毒活性，以及程序性细胞死亡蛋白1PD-1与其配体PD-L1之间相互作用的抑制作用也被评估。
