Synthesis and biological evaluation of novel farnesylthiosalicylic acid/hydro-xylcinnamic acid hybrids as potential antitumor agents

WANG Zhiqiang; WANG Xuemin; ZHANG Wei; WANG Xinyang; LING Yong; CHEN Li

doi:10.11665/j.issn.1000-5048.20140402

Journal of China Pharmaceutical University > 2014 > 45(4): 392-399. > DOI: 10.11665/j.issn.1000-5048.20140402

WANG Zhiqiang, WANG Xuemin, ZHANG Wei, WANG Xinyang, LING Yong, CHEN Li. Synthesis and biological evaluation of novel farnesylthiosalicylic acid/hydro-xylcinnamic acid hybrids as potential antitumor agents[J]. Journal of China Pharmaceutical University, 2014, 45(4): 392-399. DOI: 10.11665/j.issn.1000-5048.20140402

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Synthesis and biological evaluation of novel farnesylthiosalicylic acid/hydro-xylcinnamic acid hybrids as potential antitumor agents

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Abstract

Novel hybrid compounds 7a-7p were designed and synthesized via conjugating farnesylthiosalicylic acid(FTS)and hydroxylcinnamic acids, and their in vitro biological activities were evaluated. It was found that most compounds displayed good to moderate in vitro antitumor activities against six human cancer cells. Especially, the antitumor activities of compound 7b , with the IC₅₀ values of 5. 51-9. 25 μmol/L range against all tested cancer cells, were superior to those of FTS and sorafenib, and compound 7b could selectively inhibit the proliferation of tumor cells but not that of human normal cell. Furthermore, compound 7b significantly induced SMMC-7721 cell apoptosis in a dose-dependent manner.
- farnesylthiosalicylic acid,
- hydroxylcinnamic acids,
- synthesis,
- cell apoptosis,
- antitumor activity

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Synthesis and biological evaluation of novel farnesylthiosalicylic acid/hydro-xylcinnamic acid hybrids as potential antitumor agents

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