2,3-取代喹喔啉-6-胺类似物的抗增殖作用：构效关系研究。
2,3-Substituted quinoxalin-6-amine analogs as antiproliferatives: a structure-activity relationship study.
机构信息
Eppley Institute for Cancer Research, University of Nebraska Medical Center, Omaha, NE 68198, United States.
出版信息
Bioorg Med Chem Lett. 2011 Apr 1;21(7):1929-32. doi: 10.1016/j.bmcl.2011.02.055. Epub 2011 Feb 17.
Abstract
The quinoxaline core is considered a privileged scaffold as it is found in a variety of biologically relevant molecules. Here we report the synthesis of a quinoxalin-6-amine library, screening against a panel of cancer cell lines and a structure-activity relationship (SAR). This resulted in the identification of a bisfuranylquinoxalineurea analog (7c) that has low micromolar potency against the panel of cancer cell lines. We also show that cells treated with quinoxalineurea 7c results in caspase 3/7 activation, PARP cleavage and Mcl-1 dependent apoptosis.
摘要
喹喔啉核心被认为是一种特权支架，因为它存在于各种具有生物相关性的分子中。在这里，我们报告了喹喔啉-6-胺文库的合成，对一系列癌细胞系进行了筛选，并进行了构效关系（SAR）研究。这导致发现了一种双呋喃基喹喔啉脲类似物（7c），它对癌细胞系具有低微摩尔效力。我们还表明，用喹喔啉脲 7c 处理的细胞会导致 caspase 3/7 激活、PARP 切割和 Mcl-1 依赖性细胞凋亡。
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