Ren Tieshun, Lv Ke, Hu Fangzhong, Chen Yue
State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, Nankai University, Tianjin 300350, People's Republic of China.
State Key Laboratory and Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, People's Republic of China.
Org Biomol Chem. 2025 Feb 12;23(7):1569-1573. doi: 10.1039/d4ob01409j.
The total synthesis of Kavaratamide A, a new Linear Lipodepsipeptide from the Marine Cyanobacterium was achieved by assembling the side chain in stage through condensation coupling, carbon-chain extension, Steglich esterification and Evans aldol reaction. In addition, total synthesis of Kavaratamide A's isomer, 5--kavaratamide A, is also successfully achieved. Cytotoxicity test suggested that Kavaratamide A and 5--Kavaratamide A have a moderate bioactivity against cancer cells.
从海洋蓝细菌中分离得到的一种新型线性脂缩肽——卡瓦拉酰胺A的全合成，是通过在各个阶段通过缩合偶联、碳链延长、施陶丁格酯化反应和埃文斯羟醛反应来组装侧链而实现的。此外，卡瓦拉酰胺A的异构体5-卡瓦拉酰胺A的全合成也成功完成。细胞毒性测试表明，卡瓦拉酰胺A和5-卡瓦拉酰胺A对癌细胞具有中等生物活性。
