当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > 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.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Blackburn C,Barrett C,Brunson M,Chin J,England D,Garcia K,Gigstad K,Gould A,Gutierrez J,Hoar K,Rowland RS,Tsu C,Ringeling J,Wager K,Xu H

doi

10.1016/j.bmcl.2014.10.022

subject

Has Abstract

pub_date

2014-12-01 00:00:00

pages

5450-4

issue

23

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)01067-1

journal_volume

24

pub_type

杂志文章

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