Startseite Lebenswissenschaften Design, synthesis and evaluation of antitumor activity of new rotundic acid acylhydrazone derivatives
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Design, synthesis and evaluation of antitumor activity of new rotundic acid acylhydrazone derivatives

  • Yu-Fang He , Min-Lun Nan , Yu-Wei Zhao , Wen-Yi Sun , Wei Li EMAIL logo und Quan-cheng Zhao
Veröffentlicht/Copyright: 11. Mai 2016

Abstract

In light of the important antitumor activity of acylhydrazone compounds and based on our previous study, 18 new rotundic acid (RA) acylhydrazone derivatives were synthesized. All of the compounds were characterized by their spectroscopic data. The antiproliferative activity of the compounds was evaluated in vitro via the MTT method in three tumor cell lines, including A-375 (human malignant melanoma cells), SPC-A1 (human lung adenocarcinoma) and NCI-H446 (small cell lung cancer). The results showed that the antiproliferative activity of all of the compounds on the NCI-H446 cell line did not increase compared to RA, however, most of the derivatives exhibited higher activity against the A375 and SPC-A1 cell lines as compared to RA. Importantly, the antiproliferative activities of compounds 5a and 5b were the highest among the compounds, with IC50 values <10 μM. Collectively, compounds 5a and 5b may act as potential anti-tumor agents in the future.

Award Identifier / Grant number: 31470418

Funding statement: This work was supported by grant of the National Natural Science Foundation of China (No. 31470418).

Acknowledgments:

This work was supported by grant of the National Natural Science Foundation of China (No. 31470418).

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Received: 2015-4-29
Revised: 2016-3-16
Accepted: 2016-4-13
Published Online: 2016-5-11
Published in Print: 2016-5-1

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