Mathew Bini, Hobrath Judith V, Lu Wenyan, Li Yonghe, Reynolds Robert C
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.
Med Chem Res. 2017;26(11):3038-3045. doi: 10.1007/s00044-017-2001-z. Epub 2017 Aug 5.
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.
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。
