Potent histone deacetylase inhibitors:: N-hydroxybenzamides with antitumor activities
Potent histone deacetylase inhibitors:: N-hydroxybenzamides with antitumor activities
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DOI：
10.1016/j.bmc.2004.06.020
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发表时间：
2004-08-15
影响因子：
3.5
通讯作者：
Uesato, S
中科院分区：
文献类型：
--
作者：
Maeda, T;Nagaoka, Y;Uesato, S
对N-羟基苯甲酰胺类化合物的HDAC抑制活性进行了筛选试验，发现了具有2-萘基羰基和1，4-联苯羰基的有前途的化合物。这些化合物被进一步修饰以优化其物理化学特征。结果，获得了具有6-氨基-2-萘基羰基的抑制剂，其不仅显示出对一组肿瘤细胞的有希望的生长抑制，而且还显示出改善的水溶性。在P388细胞接种小鼠的体内实验中，它表现出最大185%的存活率（%T/C）。(C)2004 Elsevier Ltd.保留所有权利。
The screening tests of N-hydroxybenzamides for their HDAC-inhibitory activities led to the discovery of the promising compounds with a 2-naphthylcarbonyl group and with a 1,4-biphenylcarbonyl group. These compounds were further modified to optimize their physico-chemical profile. As a result, the inhibitor with a 6-amino-2-naphthylcarbonyl was obtained, which showed not only promising growth inhibitions against a panel of tumor cells, but also an improved water solubility. It exhibited the maximal 185% of survival rate (%T/C) in a in vivo experiment with P388 cell-inoculated mice. (C) 2004 Elsevier Ltd. All rights reserved.