Design, synthesis, inhibiting HDACs ability and antitumor activity of pyrimidin-4(3H)-one hydroxamate derivatives

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• 作者：Haibin Lu ; Xiangqun Jin ; Yang Jin…
• 刊名：Chemical Research in Chinese Universities
• 出版年：2016
• 出版时间：August 2016
• 年：2016
• 卷：32
• 期：4
• 页码：576-580
• 全文大小：310 KB
• 刊物主题：Chemistry/Food Science, general; Analytical Chemistry; Inorganic Chemistry; Organic Chemistry; Physical Chemistry;
• 出版者：Springer Berlin Heidelberg
• ISSN：2210-3171
• 卷排序：32

文摘

A series of novel pyrimidin-4(3H)-one hydroxamate derivatives was designed, synthesized and studied for their activities against histone deacetylases(HDACs). The results indicate that all the compounds show HDACs inhibitiory activity. The antiproliferative activities of the compounds against HeLa and A549 cells were also investigated. The pharmacological results show compound 9g has potent activity in the enzymatic inhibition assay and cell-based assay.KeywordsHistone deacetylasesAntitumor acitivtyPyrimidin-4(3H)-one hydroxamate derivative