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Discovery of Multi-target Anticancer Agents Based on HDAC Inhibitor MS-275 and 5-FU

[ Vol. 12 , Issue. 1 ]


Yuqi Jiang, Xiaoguang Li, Xiaoyang Li, Jinning Hou, Yongzheng Ding, Jian Zhang, Wenfang Xu and Yingjie Zhang   Pages 30 - 36 ( 7 )


Histone deacetylases (HDACs) inhibitors have multiple effects targeting the cancer cells and have become one of the promising cancer therapeutics with possibly broad applicability. Combination of HDAC inhibitors with the cytotoxic fluorouracil (5-FU) showed additive and synergistic effects both in vitro and in vivo. To explore the possibility in cancer therapy of a bivalent agent that combines two bioactive groups within a single molecular architecture, we designed and synthesized new dual-acting compounds by combining the bioactive fragment of MS-275, a clinical HDACs inhibitor, with cytotoxic agent 5-FU. The target compounds 9a and 9b showed comparable HDACs inhibition with MS-275 and moderate antiproliferative acitivities against six cancer cells lines.


Anticancer, HDAC, MS-275, Multitarget, 5-Fluorouracil.


Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, 250012 Ji’nan, Shandong, PR China.

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