Synthesis and evaluation of 4-(2-hydroxypropyl)piperazin-1-yl) derivatives as Hsp90 inhibitors
Synthesis and evaluation of 4-(2-hydroxypropyl)piperazin-1-yl) derivatives as Hsp90 inhibitors
复制标题
4-(2-羟丙基)哌嗪-1-基)衍生物的合成及Hsp90抑制剂的评价
DOI：
10.1016/j.bmc.2016.03.049
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发表时间：
2016-06-01
影响因子：
3.5
通讯作者：
You, Qi-Dong
中科院分区：
文献类型：
--
作者：
Cherfaoui, Bahidja;Guo, Tian-kun;You, Qi-Dong
我们先前报道了4-(3-((6-bromonaphthalen-2-yl)oxy)-2-hydroxypropyl)-N，N-二甲基哌嗪-1-磺酰胺(1)是一种新的具有中等活性的热休克蛋白90抑制剂。在我们发现Hsp90调节剂的持续努力中，我们对1进行了结构研究。设计、合成和评价了一系列标题为Hsp90的化合物。我们发现，哌嗪部分芳环上C-4位含羟基的化合物具有Hsp90抑制活性。活性较高的化合物6f可进一步开发和优化为Hsp90抑制剂。(C)2016爱思唯尔有限公司。保留所有权利。
We previously reported 4-(3-((6-bromonaphthalen-2-yl)oxy)-2-hydroxypropyl)-N,N-dimethylpiperazine- 1-sulfonamide (1) as a novel heat shock protein 90 inhibitor with moderate activity. In our ongoing efforts for the discovery of Hsp90 modulators we undertake structural investigations on 1. Series of the titled compound were designed, synthesized and evaluated. We have found that compounds with a hydroxyl group at C-4 of the aryl ring on the piperazine moiety possess Hsp90 inhibition properties. Compound 6f with improved activity could be further developed and optimized as Hsp90 inhibitor. (C) 2016 Elsevier Ltd. All rights reserved.