New method for synthesis of EZH2 methyltransferase inhibitor GSK126

被引：3

作者：

Lu, Chen ^{[1
]}

Zhang, Qiang ^{[1
]}

Chen, Xin ^{[1
]}

机构：

[1] Changzhou Univ, Sch Pharmaceut Engn & Life Sci, Changzhou 213164, Jiangsu, Peoples R China

来源：

SYNTHETIC COMMUNICATIONS | 2016年 / 46卷 / 14期

基金：

美国国家科学基金会;

关键词：

EZH2; methyltransferase; GSK126; inhibitor; synthesis; POLYCOMB GROUP PROTEIN; LYSINE METHYLTRANSFERASES; H3K27; METHYLATION; LYMPHOMA; CANCER; CELLS;

D O I：

10.1080/00397911.2016.1193875

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

GSK126 is a potent small-molecule inhibitor of S-adenosyl-methionine-competitive EZH2 methyltransferase and has the potential to be used clinically for preventing unwanted histone methylation of tumor suppressor genes. In this article, we describe a new synthetic route that has been developed for synthesizing the title compound through nine steps, starting from 2,5-dibromobenzoic acid. This synthetic method is economical and suitable for multigram-scale preparation of GSK126 and related N-alkylated indole derivatives. [GRAPHICS]

引用

页码：1215 / 1222

页数：8

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