A series of triazolo-pyridazinone derivatives were prepared through the standard
click reactions of 4,6-diphenyl-2-(prop-2-yn-1-yl)pyridazin-3(2H)-one 1, possessing
a free terminal alkyne group with a selection of substituted aryl azides 2-9. The cytotoxicity
and in vitro anticancer investigation of the new compounds were conducted against
four different human tumor cell lines, including breast adenocarcinoma MCF-7, hepatocellular
carcinoma HepG2, lung cancer A549 and colon cancer HCT116 cell lines. The
results showed that the compounds exerted their actions in MCF-7 and A549 via inhibition
of the urokinase activity. The compound 17 showed potent anticancer activity compared
with the activity of the standard anticancer drug, doxorubicin. Molecular docking
studies were performed to support the activity data and predict the plausible mechanisms
of the ligand-protein interactions.
Keywords: Trizolo-pyridazinone, anticancer, urokinase, MCF-7, HepG2, A549, HCT116.
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