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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 13, Issue 8, 2016

Page: [729 - 733] Pages: 5

DOI: 10.2174/157018081308160826182531

Price: $65


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.

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

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