2,3-Substituted quinoxalin-6-amine analogs as antiproliferatives: A structure-activity relationship study
2,3-Substituted quinoxalin-6-amine analogs as antiproliferatives: A structure-activity relationship study
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DOI：
10.1016/j.bmcl.2011.02.055
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发表时间：
2011-04-01
影响因子：
2.7
通讯作者：
Natarajan, Amarnath
中科院分区：
文献类型：
--
作者：
Chen, Qianyi;Bryant, Vashti C.;Natarajan, Amarnath
喹喔啉核心被认为是一种特殊的支架，因为它存在于多种生物相关分子中。在这里，我们报告了喹喔啉-6-胺文库的合成、针对一组癌细胞系的筛选和构效关系（SAR）。由此鉴定出双呋喃基喹喔啉脲类似物 (7c)，该类似物对一组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 裂解和 Mcl-1 依赖性细胞凋亡。 (C) 2011 Elsevier Ltd. 保留所有权利。
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. (C) 2011 Elsevier Ltd. All rights reserved.