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MAO Chunfang, XU Chenjun, WANG Xuemin, LI Xianghua, ZHANG Wei, WANG Xinyang, LING Yong. Design, synthesis and antitumor activity of farnesylthiosalicylamide derivatives[J]. Journal of China Pharmaceutical University, 2015, 46(2): 162-168. DOI: 10.11665/j.issn.1000-5048.20150204
Citation: MAO Chunfang, XU Chenjun, WANG Xuemin, LI Xianghua, ZHANG Wei, WANG Xinyang, LING Yong. Design, synthesis and antitumor activity of farnesylthiosalicylamide derivatives[J]. Journal of China Pharmaceutical University, 2015, 46(2): 162-168. DOI: 10.11665/j.issn.1000-5048.20150204
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Design, synthesis and antitumor activity of farnesylthiosalicylamide derivatives

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  • A series of farnesylthiosalicylamide derivatives( 9a-9k )were designed and synthesized via condensating the carboxyl of farnesylthiosalicylic acid(FTS)with different amines, and the in vitro biological activity was evaluated. It was observed that eight of them displayed strong antitumor activity against five human cancer cells in vitro. Notably, compound 9k exhibited the most active with the IC50 values of 6. 05-8. 16 μmol/L range against the tested cancer cells, which were superior to those of FTS and even comparable to that of sorafenib in vitro. In addition, compound 9k down-regulated the protein of Bcl-2 and increased the expression levels of Bax and caspase-3 proteins, indicating that compound 9k could induce tumor cell apoptosis.
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