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Synthesis and Biological Evaluation of Novel 1,3,4-thiadiazole Derivatives Incorporating Benzisoselenazolone Scaffold as Potential Antitumor Agents

[ Vol. 12 , Issue. 7 ]


Xiaoyun Fu, Sha Li, Fen Jing, Xuefeng Wang, Baolin Li, Jijun Zhao, Yuming Liu and Baoquan Chen   Pages 631 - 639 ( 9 )


Background: Based on the biological signi cance of benzisoselenazolone and 1,3,4-thiadiazole, a series of novel 1,3,4-thiadiazole derivatives incorporating benzisoselenazolone scaffold were designed and synthesized with ebselen as a lead compound.

Methods: Meanwhile, their in vitro antitumor activities were evaluated against SMMC-7721, MCF-7 and A549 human cancer cell lines by CCK-8 assay.

Results: The preliminary bioassay results demonstrated that all tested compounds 4a-q showed potent antitumor activities, and some compounds exhibited better effects than positive control ethaselen and 5-fluorouracil (5-FU) against various cancer cell lines. Furthermore, compounds 4b and 4m showed significant antitumor activities against SMMC-7721 cells with IC50 values of 1.89 and 1.89 M, respectively. Compounds 4c and 4n displayed highly effective biological activities against MCF-7 cells with IC50 values of 2.88 and 2.28 M, respectively. Compound 4i showed the best inhibitory effect against A549 cells with IC50 value of 1.76 M.

Conclusion: The pharmacological results suggest that the substituent groups of phenyl ring on the 1,3,4-thiadiazole are vital for modulating antitumor activities against various cancer cell lines.


1, 3, 4-Thiadiazole derivatives, benzisoselenazolone, ebselen, ethaselen, antitumor activity.


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

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