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引用本文的文献

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Insights into the structure-activity relationship of the anticancer compound ZJ-101: A role played by the amide moiety.抗癌化合物 ZJ-101 的结构-活性关系研究：酰胺部分的作用。
Bioorg Med Chem Lett. 2024 Jun 1;105:129741. doi: 10.1016/j.bmcl.2024.129741. Epub 2024 Apr 9.
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本文引用的文献

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Insights into the structure-activity relationship of the anticancer compound ZJ-101: A critical role played by the cyclohexene ring.抗癌化合物ZJ-101的构效关系研究：环己烯环发挥的关键作用
Bioorg Med Chem Lett. 2016 Jun 15;26(12):2890-2892. doi: 10.1016/j.bmcl.2016.04.044. Epub 2016 Apr 19.
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Design, synthesis, and biological evaluation of truncated superstolide A.截短型超级斯托利德A的设计、合成及生物学评价
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海洋天然产物超斯托利德A衍生物抗癌化合物ZJ-101的构效关系研究：共轭三烯内酯部分发挥的关键作用。

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.

作者信息

Qian Shan, Shah Aashay K, Head Sarah A, Liu Jun O, Jin Zhendong

机构信息

Department of Pharmaceutical Sciences and Experimental Therapeutics, College of Pharmacy, The University of Iowa, Iowa City, IA 52242, USA.

Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, 725 North Wolfe St., Baltimore, MD 21205, USA.

出版信息

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3411-3. doi: 10.1016/j.bmcl.2016.06.057. Epub 2016 Jun 22.

DOI:10.1016/j.bmcl.2016.06.057
PMID:27374243
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5013146/
Abstract

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.

摘要

化合物ZJ - 101是海洋天然产物超斯托利德A的结构简化类似物，此前由我们实验室研发。在随后的构效关系研究中，设计并合成了两种新的类似物ZJ - 105和ZJ - 106，通过将ZJ - 101中的C2 - C3双键替换为单键，并将ZJ - 101中C4 - C5双键的构型从Z型转变为E型，来探究分子中共轭三烯内酯部分的重要性。生物学评价表明，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明显低于ZJ - 101，这表明该分子的共轭三烯内酯部分对其抗癌活性至关重要。