Design, Synthesis and Biological Evaluation of Novel Tamibarotene Derivative as Multitarget Anticancer Agent

Title:Design, Synthesis and Biological Evaluation of Novel Tamibarotene Derivative as Multitarget Anticancer Agent

Volume: 13 Issue: 8

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

Affiliation:

Keywords: Tamibarotene (AM80), multitarget, 5-fluorouracil (5-FU), anticancer, leukemia.

Abstract: A novel tamibarotene derivative was synthesized by coupling cytotoxic agent 5-Fluorouracil (5-FU) with tamibarotene via ester. This hybrid drug (compound 10) was evaluated for its antiproliferative activities against human leukemic U937, HL-60 and K562 cell lines in vitro. Results showed that compound 10 exhibited more potent anti-leukemic activity than the positive control tamibarotene. Furthermore, the preliminary stability test of compound 10 revealed that it could release tamibarotene and 5-FU significantly in vitro. These interesting results would be meaningful to develop more potent drugs for the treatment of human leukemia.

Cite this article as:

Jiang Yuqi, Hou Jinning, Li Xiaoyang, Xu Wenfang and Zhang Yingjie, Design, Synthesis and Biological Evaluation of Novel Tamibarotene Derivative as Multitarget Anticancer Agent, Letters in Drug Design & Discovery 2016; 13(8) . https://dx.doi.org/10.2174/157018081308160826182531