Background: A series of symmetrical 1,4-disubstituted bis-1,2,3-triazoles was prepared by
double copper catalyzed Azide-alkyne Cycloaddition (CuAAC) from aliphatic bis-azides and a
tetraethylene glycol bis-azide derivative. The eighteen novel compounds were evaluated in vitro for their
cytotoxic activity against two human tumor cell lines: Human breast adenocarcinoma (MDA-MB 231)
and ovarian adenocarcinoma (TOV-21G).
Results and Conclusion: The results of colorimetric MTT assays showed that compounds 4j and 4q
exhibited a better selectivity index and cell viability comparable with the standard drug doxorubicin.
These compounds induced apoptosis in both tested cell lines, as assessed by BrdU assay. The results
suggest that these structurally simple compounds may be promising prototypes for antitumoral agents.
Keywords: Symmetrical bis-1, 2, 3-triazoles, Bis-azides, Double CuAAC, Cytotoxicity, BrdU, Apoptosis, Cancer.
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