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

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

Volume: 12 Issue: 1

Author(s): Yuqi Jiang, Xiaoguang Li, Xiaoyang Li, Jinning Hou, Yongzheng Ding, Jian Zhang, Wenfang Xu and Yingjie Zhang

Affiliation:

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

Abstract: 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.

Cite this article as:

Jiang Yuqi, Li Xiaoguang, Li Xiaoyang, Hou Jinning, Ding Yongzheng, Zhang Jian, Xu Wenfang and Zhang Yingjie, Discovery of Multi-target Anticancer Agents Based on HDAC Inhibitor MS-275 and 5-FU, Medicinal Chemistry 2016; 12 (1) . https://dx.doi.org/10.2174/1573406411666150714111045