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新型异噁唑基 HDAC 抑制剂的设计与合成。

Design and synthesis of novel isoxazole-based HDAC inhibitors.

机构信息

Dipartimento di Scienze Farmaceutiche Pietro Pratesi, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy.

出版信息

Eur J Med Chem. 2010 Sep;45(9):4331-8. doi: 10.1016/j.ejmech.2010.06.035. Epub 2010 Jun 30.

Abstract

A series of isoxazole-based histone deacetylase (HDAC) inhibitors structurally related to SAHA were designed and synthesized. The isoxazole moiety was inserted in the vicinity of the Zn(2+)-binding group in order to check its participation in the coordinating process.

摘要

设计并合成了一系列与 SAHA 结构相关的基于异噁唑的组蛋白去乙酰化酶 (HDAC) 抑制剂。将异噁唑部分插入 Zn(2+)-结合基团附近,以检查其在配位过程中的参与。

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