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Synthesis and in vitro antiproliferative activity of novel benzisoselenazolone derivatives

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Abstract

A series of novel benzisoselenazolone derivatives bearing 1,3,4-thiadiazole moiety were designed, synthesized and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, MCF-7, A549, and normal cell lines L929 by CCK-8 assay. The bioassay results demonstrated that most of the tested compounds showed potent antitumor activities, and some compounds exhibited better effects than positive control ebselen and ethaselen against various cancer cell lines. Among these compounds, compound 7l showed significant antiproliferative activity against SMMC-7721 cells, with IC50 values of 2.18 μM. Compound 7j exhibited the best inhibitory effect against MCF-7 cells, with IC50 values of 2.89 μM. Compounds 7e and 7i displayed highly effective antitumor activities against A549 cells, with IC50 values of 2.33 and 2.33 μM, respectively. Furthermore, most of the tested compounds showed weak cytotoxic effect against the normal cell lines L929. The pharmacological results suggest that the substituents of benzoylmethylthio-moiety at position-2 on 1,3,4-thiadiazole are vital for modulating antiproliferative activities against various tumor cell lines.

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Acknowledgments

We are grateful to the National Natural Science Foundation of China (20971097) and Tianjin Municipal Natural Science Foundation (13JCYBJC24500) for financial support.

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The authors declare that they have no conflict of interest.

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Authors and Affiliations

  1. School of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin, 300384, China

    Li-na Xuan, Peng Wang, Kai Zhang, Yan-ping Shi, Yu-ming Liu, Tao Zhu & Bao-quan Chen

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  1. Li-na Xuan
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  2. Peng Wang
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  3. Kai Zhang
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  4. Yan-ping Shi
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  5. Yu-ming Liu
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Correspondence to Bao-quan Chen.

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Xuan, Ln., Wang, P., Zhang, K. et al. Synthesis and in vitro antiproliferative activity of novel benzisoselenazolone derivatives. Med Chem Res 24, 543–552 (2015). https://doi.org/10.1007/s00044-014-1149-z

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