Design, synthesis and evaluation of belinostat analogs as histone deacetylase inhibitors

被引：5

作者：

Zhang, Jie-Huan ^{[1
]}

Mottamal, Madhusoodanan ^{[3
,4
]}

Jin, Hai-Shan ^{[1
]}

Guo, Shanchun ^{[3
,4
]}

Gu, Yan ^{[1
]}

Wang, Guangdi ^{[3
,4
]}

Zhao, Li-Ming ^{[1
,2
]}

机构：

[1] Jiangsu Normal Univ, Sch Chem & Mat Sci, Xuzhou 221116, Jiangsu, Peoples R China

[2] Guangxi Normal Univ, State Key Lab Chem & Mol Engn Med Resources, Guilin 541004, Guangxi, Peoples R China

[3] Xavier Univ Louisiana, RCMI Canc Res Ctr, New Orleans, LA 70125 USA

[4] Xavier Univ Louisiana, Dept Chem, New Orleans, LA 70125 USA

来源：

FUTURE MEDICINAL CHEMISTRY | 2019年 / 11卷 / 21期

关键词：

anticancer activities; drug design; molecular docking; structure-activity relationship; synthesis; HYDROXAMIC ACID; BIOLOGICAL EVALUATION; DERIVATIVES;

D O I：

10.4155/fmc-2018-0587

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aim: Histone deacetylase (HDAC) is an attractive target for antitumor therapy. Therefore, the development of novel HDAC inhibitors is warranted. Materials & methods: A series of HDAC inhibitors based on N-hydroxycinnamamide fragment was designed as the clinically used belinostat analog using amide as the connecting unit. All target compounds were evaluated for their in vitro HDAC inhibitory activities and some selected compounds were tested for their antiproliferative activities. Conclusion: Among them, compound 7e showed an IC50 value of 11.5 nM in inhibiting the HDAC in a pan-HDAC assay, being the most active compound of the series.

引用

页码：2765 / 2778

页数：14

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