Inhibitors of human histone deacetylase: Synthesis and enzyme and cellular activity of straight chain hydroxamates
Inhibitors of human histone deacetylase: Synthesis and enzyme and cellular activity of straight chain hydroxamates
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DOI：
10.1021/jm015568c
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发表时间：
2002-02-14
影响因子：
7.3
通讯作者：
Walker, H
中科院分区：
文献类型：
--
作者：
Remiszewski, SW;Sambucetti, LC;Walker, H
组蛋白去乙酰化酶（HDAC）抑制剂已被证明能诱导人肿瘤细胞系的终末分化，并在体内具有抗肿瘤作用。我们制备了亚甲基苯胺羟肟酸（SAHA）和曲古菌素A的类似物，并在人类HDAC酶抑制实验、p21(waf1) （p21）启动子实验和单层生长抑制实验中对它们进行了评估。一种化合物，4-（二甲氨基）- n -[7-（羟氨基）-7-氧庚基]-苯甲酰胺，被发现对8种人类肿瘤细胞系的生长有不同的影响。
Inhibitors of histone deacetylase (HDAC) have been shown to induce terminal differentiation of human tumor cell lines and to have antitumor effects in vivo. We have prepared analogues of suberoylanilide hydroxamic acid (SAHA) and trichostatin A and have evaluated them in a human HDAC enzyme inhibition assay, a p21(waf1) (p21) promoter assay, and in monolayer growth inhibition assays. One compound, 4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]-benzamide, was found to affect the growth of a panel of eight human tumor cell lines differentially.