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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Insights into the structure-activity relationship of the anticancer compound ZJ-101, a derivative of marine natural product superstolide A: A critical role played by the conjugated trienyl lactone moiety
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Insights into the structure-activity relationship of the anticancer compound ZJ-101, a derivative of marine natural product superstolide A: A critical role played by the conjugated trienyl lactone moiety

机译：海洋天然产物超级杀菌素A的抗癌化合物ZJ-101的构效关系的见解：共轭三烯基内酯部分起着关键作用

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摘要

Compound ZJ-101, a structurally simplified analog of the marine natural product superstolide A, was previously developed in our laboratory. In the subsequent structure-activity relationship study, two new analogs, ZJ-105 and ZJ-106, were designed and synthesized to probe the importance of the conjugated trienyl lactone moiety of the molecule by replacing the C2-C3 double bond in ZJ-101 with a single bond and switching the geometry of the C4-C5 double bond in ZJ-101 from Z to E, respectively. Biological evaluation showed that ZJ-105 completely loses antiproliferative activity whereas ZJ-106 is significantly less active against cancer cells in vitro than ZJ-101, suggesting that the conjugated trienyl lactone moiety of the molecule is critical for its anticancer activity. (C) 2016 Elsevier Ltd. All rights reserved.
机译：化合物ZJ-101是海洋天然产物超杀菌素A的结构简化类似物，以前是在我们的实验室中开发的。在随后的结构-活性关系研究中，设计并合成了两个新的类似物ZJ-105和ZJ-106，以通过取代ZJ-101中的C2-C3双键来探索分子中共轭三烯内酯部分的重要性用单键将ZJ-101中C4-C5双键的几何形状分别从Z切换到E。生物学评估表明，ZJ-105完全丧失了抗增殖活性，而ZJ-106在体外对癌细胞的活性远低于ZJ-101，这表明该分子的共轭三烯基内酯部分对其抗癌活性至关重要。 （C）2016 Elsevier Ltd.保留所有权利。

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