Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors

doi:10.1021/ml400470s

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	Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors
	Chen, Fei; Chai, Hui; Su, Ming-Bo; Zhang, Yang-Ming; Li, Jia; Xie, Xin; Nan, Fa-Jun
刊名	ACS MEDICINAL CHEMISTRY LETTERS
	2014-06
卷号	5 期号:6 页码:628-633
关键词	Histone deacetylase inhibitors largazole bisthiazole
ISSN号	1948-5875
DOI	10.1021/ml400470s
文献子类	Article
英文摘要	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.
资助项目	National Natural Science Foundation of China[30725049] ; National Natural Science Foundation of China[81021062] ; National Natural Science Foundation of China[81072652] ; Chinese Academy of Sciences[XDA01040301] ; Ministry of Science and Technology of China[2009CB940900] ; Shanghai Science and Technology Committee[11431921102]
WOS关键词	T-CELL LYMPHOMA ; EXPERIMENTAL AUTOIMMUNE ENCEPHALOMYELITIS ; CONCISE TOTAL-SYNTHESIS ; BIOLOGICAL EVALUATION ; LARGAZOLE ANALOGS ; MULTIPLE-SCLEROSIS ; HDAC INHIBITORS ; TRICHOSTATIN-A ; DERIVATIVES ; SAHA
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000337497200005
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277043]
专题	国家新药筛选中心中科院受体结构与功能重点实验室新药研究国家重点实验室药物安全性评价中心
通讯作者	Li, Jia
作者单位	Shanghai Inst Mat Med, Chinese Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Chen, Fei,Chai, Hui,Su, Ming-Bo,et al. Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors[J]. ACS MEDICINAL CHEMISTRY LETTERS,2014,5(6):628-633.
APA	Chen, Fei.,Chai, Hui.,Su, Ming-Bo.,Zhang, Yang-Ming.,Li, Jia.,...&Nan, Fa-Jun.(2014).Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors.ACS MEDICINAL CHEMISTRY LETTERS,5(6),628-633.
MLA	Chen, Fei,et al."Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors".ACS MEDICINAL CHEMISTRY LETTERS 5.6(2014):628-633.