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Design,Synthesis, Inhibiting HDACs Ability and Antitumor Activity of Pyrimidin-4(3H)-one Hydroxamate Derivatives |
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| Authors: | LU Haibin JIN Xiangqun JIN Yang HUANG Bangrui WANG Cheng WANG Chunhe MA Fangyuan CHEN Yuting LI Jiarui CONG Yu WANG Wenlong SONG Yuming MU Xupeng |
| Affiliation: | 1. College of Pharmacy, Jilin University, Changchun 130021, P. R. China; 2. China-Japan Union Hospital of Jilin University, Changchun 130033, P. R. China |
| 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 deacetylase Antitumor acitivty Pyrimidin-4(3H)-one hydroxamate derivative |
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