Synthesis and antitumor evaluation of novel fused heterocyclic 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole derivatives
- Tianjin University of Technology, School of Chemistry and Chemical Engineering, Tianjin Key Laboratory of Organic Solar Cells And Photochemical Conversion (China)
In this study, twenty three 3,6-disubstituted 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole derivatives were synthesized and their antiproliferative activities in vitro were studied against SMMC-7721, HeLa, A549, and L929 by the CCK-8 assay. The bioassay results demonstrated that all tested compounds 8(a–w) exhibited antiproliferation with different degrees, and some compounds showed better effects than reference drug 5-fluorouracil. Among these screened compounds, compounds 8a, 8d, and 8l displayed significant antitumor activities in inhibiting SMMC-7721cell proliferation with IC{sub 50} values of 1.64, 1.74, and 1.61 µM, respectively. Compounds 8d and 8l were manifested highly effective biological activity versus HeLa cells with IC{sub 50} values of 2.23 and 2.84 µM, respectively. Compound 8l was found to have the highest antitumor potency against A549 cells with IC{sub 50} value of 2.67 µM. Furthermore, all compounds exhibited weaker cytotoxic effects than 5-fluorouracil on normal cell lines L929.
- OSTI ID:
- 22936168
- Journal Information:
- Medicinal Chemistry Research (Print), Vol. 28, Issue 10; Other Information: Copyright (c) 2019 Springer Science+Business Media, LLC, part of Springer Nature; Country of input: International Atomic Energy Agency (IAEA); ISSN 1054-2523
- Country of Publication:
- United States
- Language:
- English
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