Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors

被引：31

作者：

Chen, Fei ^{[1
]}

Chai, Hui ^{[1
]}

Su, Ming-Bo ^{[1
]}

Zhang, Yang-Ming ^{[1
]}

Li, Jia ^{[1
]}

Xie, Xin ^{[1
]}

Nan, Fa-Jun ^{[1
]}

机构：

[1] Shanghai Inst Mat Med, Chinese Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2014年 / 5卷 / 06期

基金：

中国国家自然科学基金;

关键词：

Histone deacetylase inhibitors; largazole; bisthiazole; CONCISE TOTAL-SYNTHESIS; HDAC INHIBITORS; BIOLOGICAL EVALUATION; LARGAZOLE ANALOGS; TRICHOSTATIN-A; DERIVATIVES; SAHA; INDUCTION; MECHANISM; APOPTOSIS;

D O I：

10.1021/ml400470s

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inspired by the thiazole thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be orally efficacious in ameliorating clinical symptoms of EAE mice.

引用

页码：628 / 633

页数：6

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