Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a] pyrazine and related heterocycles selective for the HDAC6 isoform
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a] pyrazine and related heterocycles selective for the HDAC6 isoform
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DOI：
10.1016/j.bmcl.2014.10.022
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发表时间：
2014-12-01
影响因子：
2.7
通讯作者：
Xu, He
中科院分区：
文献类型：
--
作者：
Blackburn, Christopher;Barrett, Cynthia;Xu, He
4-（氨甲基）-N-羟基苯甲酰胺的酰基衍生物是有效的亚型选择性HDAC 6抑制剂。基于1，2，3，4-四氢吡咯并[1，2-a]吡嗪的受约束杂环类似物显示出在细胞中进一步增强的HDAC 6选择性和抑制活性。同源性模型表明，与其他HDAC亚型相比，杂环间隔区可以更有效地进入HDAC 6的更宽的催化通道。(C)2014爱思唯尔有限公司版权所有。
Acyl derivatives of 4-(aminomethyl)-N-hydroxybenzamide are potent sub-type selective HDAC6 inhibitors. Constrained heterocyclic analogs based on 1,2,3,4-tetrahydropyrrolo[1,2-a] pyrazine show further enhanced HDAC6 selectivity and inhibitory activity in cells. Homology models suggest that the heterocyclic spacer can more effectively access the wider catalytic channel of HDAC6 compared to other HDAC sub-types. (C) 2014 Elsevier Ltd. All rights reserved.