Synthesis and antitumor activities of 1,3,4-thiadiazole derivatives possessing benzisoselenazolone scaffold

Abstract

A series of novel 1,3,4-thiadiazole derivatives possessing benzisoselenazolone scaffold were designed and synthesized, and their antitumor activities against human cervix adenocarcinoma(HeLa), human liver cancer cell(SMMC-7721), human breast cancer cell(MCF-7) and human lung cancer cell(A549) lines were evaluated by CCK-8 assay. The bioassay results demonstrate that most of the tested compounds showed potent antiproliferative effects against various cell lines. Furthermore, compounds 7c, 7e, 7h, 7i and 7k showed significant antiproliferative activities against SMMC-7721 cells, with IC₅₀ values of 2.38, 2.67, 1.35, 2.75 and 2.48 μmol/L, respectively. Compounds 7a, 7e, 7j and 7l exhibited highly effective antitumor activities against MCF-7 cells, with IC₅₀ values of 2.89, 2.95, 1.12 and 2.75 μmol/L, respectively. Compound 7j was found to be the most potent compound against A549 cells, with an IC₅₀ value of 1.25 μmol/L. The pharmacological results suggest that the substituents of benzylthio-moiety at position 2 on 1,3,4-thiadiazole are vital for modulating antitumor activities against various cancer cell lines.

Keywords

1,3,4-Thiadiazole derivative / Benzisoselenazolone / Antitumor activity

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