Biological Evaluation of New Largazole Analogues: Alteration of Macrocyclic Scaffold with Click Chemistry

被引：35

作者：

Li, Xianlin ^{[1
]}

Tu, Zhenchao ^{[1
]}

Li, Hua ^{[1
]}

Liu, Chunping ^{[1
]}

Li, Zheng ^{[2
]}

Sun, Qiao ^{[1
]}

Yao, Yiwu ^{[1
]}

Liu, Jinsong ^{[1
]}

Jiang, Sheng ^{[1
]}

机构：

[1] Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Lab Regenerat Biol, Guangzhou 510530, Guangdong, Peoples R China

[2] Methodist Hosp, Res Inst, Houston, TX 77030 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2013年 / 4卷 / 01期

关键词：

HDAC inhibitor; peptides; macrocycles; largazole; click chemistry; HISTONE-DEACETYLASE INHIBITORS; EXPRESSION; CONFORMATION; CANCER; HDACS;

D O I：

10.1021/ml300371t

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the design, synthesis, and biological evaluation of a new series of largazole analogues in which a 4-methylthiazoline moiety was replaced with a triazole and tetrazole ring, respectively. Compound 7 bearing a tetrazole ring was identified to show much better selectivity for HDAC1 over HDAC9 than largazole (10-fold). This work could serve as a foundation for further exploration of selective HDAC inhibitors using a largazole molecular scaffold.

引用

页码：132 / 136

页数：5

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