Isolation and Total Synthesis of Kinenzoline, an Antitrypanosomal Linear Depsipeptide Isolated from a Marine Salileptolyngbya sp. Cyanobacterium
Isolation and Total Synthesis of Kinenzoline, an Antitrypanosomal Linear Depsipeptide Isolated from a Marine Salileptolyngbya sp. Cyanobacterium
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DOI：
10.1021/acs.joc.1c00817
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发表时间：
2021-08-31
影响因子：
3.6
通讯作者：
Suenaga, Kiyotake
中科院分区：
文献类型：
--
作者：
Kurisawa, Naoaki;Otomo, Keisuke;Suenaga, Kiyotake
Kinenzoline (1) 是一种新的线性缩酚肽，是从海洋 Salileptolyngbya sp 中分离出来的。蓝细菌。通过光谱分析和降解反应阐明了其结构。此外，我们还实现了1的全合成并确认了其结构。与正常人体细胞（WI-38，IC50 > 100 mu M）相比，Kinenzoline (1) 对昏睡病的病原体罗得西亚布氏锥虫 (IC50 4.5 mu M) 显示出高度选择性的抗增殖活性。 Kinenzoline (1) 是一种很有前景的先导化合物，可用于开发新型抗锥虫药物。
Kinenzoline (1), a new linear depsipeptide, was isolated from a marine Salileptolyngbya sp. cyanobacterium. Its structure was elucidated by spectroscopic analyses and degradation reactions. In addition, we achieved a total synthesis of 1 and confirmed its structure. Kinenzoline (1) showed highly selective antiproliferative activity against the causative organism of sleeping sickness, Trypanosoma brucei rhodesiense (IC50 4.5 mu M), compared to normal human cells (WI-38, IC50 > 100 mu M). Kinenzoline (1) is a promising lead compound for the development of new antitrypanosomal drugs.