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

Haibin Lu; Xiangqun Jin; Yang Jin; Bangrui Huang; Cheng Wang; Chunhe Wang; Fangyuan Ma; Yuting Chen; Jiarui Li; Yu Cong; Wenlong Wang; Yuming Song; Xupeng Mu

doi:10.1007/s40242-016-6105-7

Chemical Research in Chinese Universities ›› 2016, Vol. 32 ›› Issue (4) : 576 -580. DOI: 10.1007/s40242-016-6105-7

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

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Abstract

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.

Keywords

Histone deacetylases / Antitumor acitivty / Pyrimidin-4(3H)-one hydroxamate derivative

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Haibin Lu, Xiangqun Jin, Yang Jin, Bangrui Huang, Cheng Wang, Chunhe Wang, Fangyuan Ma, Yuting Chen, Jiarui Li, Yu Cong, Wenlong Wang, Yuming Song, Xupeng Mu. Design, synthesis, inhibiting HDACs ability and antitumor activity of pyrimidin-4(3H)-one hydroxamate derivatives. Chemical Research in Chinese Universities, 2016, 32(4): 576-580 DOI:10.1007/s40242-016-6105-7

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