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非甾体抗炎药和布洛芬类小酰胺文库的抗癌及Wnt/β-连环蛋白抑制活性的合成与初步评估

Synthesis and preliminary assessment of the anticancer and Wnt/β-catenin inhibitory activity of small amide libraries of fenamates and profens.

作者信息

Mathew Bini, Hobrath Judith V, Lu Wenyan, Li Yonghe, Reynolds Robert C

机构信息

Drug Discovery Division, Southern Research Institute, 2000 Ninth Avenue South, Birmingham, AL 35205 USA.

Drug Discovery Unit, College of Life Sciences, University of Dundee, Dundee, DD1 5EH UK.

出版信息

Med Chem Res. 2017;26(11):3038-3045. doi: 10.1007/s00044-017-2001-z. Epub 2017 Aug 5.

Abstract

As part of an ongoing program to study the anticancer activity of non-steroidal anti-inflammatory drugs (NSAIDs) through generating diversity libraries of multiple NSAID scaffolds, we synthesized a series of NSAID amide derivatives and screened these sets against three cancer cell lines (prostate, colon and breast) and Wnt/β-catenin signaling. The evaluated amide analog libraries show significant anticancer activity/cell proliferation inhibition, and specific members of the sets show inhibition of Wnt/β-catenin signaling.

摘要

作为一项正在进行的通过生成多种非甾体抗炎药(NSAIDs)支架的多样化文库来研究其抗癌活性的计划的一部分,我们合成了一系列NSAID酰胺衍生物,并针对三种癌细胞系(前列腺癌、结肠癌和乳腺癌)以及Wnt/β-连环蛋白信号通路对这些化合物进行了筛选。评估的酰胺类似物文库显示出显著的抗癌活性/细胞增殖抑制作用,并且该文库中的特定成员显示出对Wnt/β-连环蛋白信号通路的抑制作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a98/5656725/e9c9a67c8ba6/44_2017_2001_Fig1_HTML.jpg

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