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布雷替菌素类似物作为抗侵袭剂的合成及构效关系研究。

Synthesis and structure-activity relationships studies of brartemicin analogs as anti-invasive agents.

机构信息

Department of Organic Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan, China.

出版信息

J Antibiot (Tokyo). 2013 Sep;66(9):531-7. doi: 10.1038/ja.2013.37. Epub 2013 May 8.

Abstract

Brartemicin is a trehalose-based inhibitor of tumor cell invasion produced by the actinomycete of the genus Nonomuraea. In order to find more potent anti-invasive agents and study the structure-activity relationships, a series of 19 brartemicin analogs were prepared via two synthetic routes from α,α-D-trehalose and evaluated for their anti-invasive activities. Compound 4f, 6,6'-bis(2,3-dimethoxybenzoyl)-α,α-D-trehalose, was more potent than the natural brartemicin. It inhibited the invasion of murine colon 26-L5, colon carcinoma SW620, melanoma B16-BL6 and breast MDA-MB-231 cells with IC50 values of 0.15, 2.35, 4.12 and 2.61 μM, respectively. Analog 4p, 6,6'-bis(3,4-dimethoxycinnamoyl)-α,α-D-trehalose, was as potent as brartemicin against invasion of murine colon 26-L5 carcinoma cells in vitro. The structure-activity relationships of these novel trehalose-based compounds were summarized.

摘要

布雷替丁菌素是一种由诺卡氏菌属放线菌产生的基于海藻糖的肿瘤细胞侵袭抑制剂。为了寻找更有效的抗侵袭剂并研究结构-活性关系,我们通过两条从α,α-D-海藻糖出发的合成路线,制备了一系列 19 种布雷替丁菌素类似物,并对它们的抗侵袭活性进行了评估。化合物 4f,6,6'-双(2,3-二甲氧基苯甲酰基)-α,α-D-海藻糖,比天然布雷替丁菌素更有效。它对鼠结肠 26-L5、结肠癌细胞 SW620、黑色素瘤 B16-BL6 和乳腺癌 MDA-MB-231 细胞的侵袭抑制活性的 IC50 值分别为 0.15、2.35、4.12 和 2.61μM。类似物 4p,6,6'-双(3,4-二甲氧基肉桂酰基)-α,α-D-海藻糖,对体外鼠结肠 26-L5 癌细胞的侵袭活性与布雷替丁菌素相当。总结了这些新型海藻糖类化合物的构效关系。

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