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Insights into the structure–activity relationship of the anticancer compound ZJ-101: A role played by the amide moiety
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2024-04-09 , DOI: 10.1016/j.bmcl.2024.129741
Haibo Qiu , Shan Qian , Sarah A. Head , Phillip R. Sanchez , Jun O. Liu , Zhendong Jin

ZJ-101, a structurally simplified analog of marine natural product superstolide A, was previously designed and synthesized in our laboratory. In the present study four new analogs of ZJ-101 were designed and synthesized to investigate the structure–activity relationship of the acetamide moiety of the molecule. The biological evaluation showed that the amide moiety is important for the molecule’s anticancer activity. Replacing the amide with other functional groups such as a sulfonamide group, a carbamate group, and a urea group resulted in the decrease in anticancer activity.

中文翻译:

深入了解抗癌化合物ZJ-101的构效关系:酰胺部分的作用

ZJ-101是我们实验室先前设计和合成的海洋天然产物superstolide A的结构简化类似物。在本研究中,设计并合成了 ZJ-101 的四种新类似物,以研究该分子乙酰胺部分的构效关系。生物学评价表明酰胺部分对该分子的抗癌活性很重要。用磺酰胺基团、氨基甲酸酯基团和脲基团等其他官能团代替酰胺会导致抗癌活性下降。
更新日期:2024-04-09
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