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A new series of trisubstituted-1,2,4-triazin-6-one derivatives (III–VIII) containing cinnmylidene and disubstituted phenyl (bearing acetoxy and methoxy) moieties have been synthesized, using 1,3-oxazolinone derivatives (IIa,b) and thiosemicarbazide as the key starting materials. The structures of the new 1,2,4-triazine-6-ones were confirmed by spectral data along with elemental microanalyses. The tittle compounds were screened for their cytotoxicity against breast cancer cell lines (MCF-7) as well as normal breast HDF. The tested 1,2,4-triazine-6-one derivatives revealed good cytotoxicity and selectivity towards breast cancer cell lines (MCF-7) relative to normal cells. Also, the compounds were tested for their potential to inhibit the activity of enzyme α-glucosidase. Meanwhile, most of the compounds exhibit the strongest enzyme inhibitory activity, while three compounds 5-cinnamylidene-3-(3,4-dimethoxy) phenyl-6(1H)-oxo-1,2,4-triazin-2-thiocarboxamide (IIIb), N-(4-chlorobenzoyl) methyl-5-cinnamylidene-6H-oxo-3-(3,4-dimethoxy) phenyl-1,2,4-triazin-3-thiocarboxamide (VI) and 5-cinnamylidene-3-(3,4-dimethoxy) phenyl-1,2,4-triazin-6-one (VIII) exhibited excellent activity with IC50 values 0.20, 0.33 and 0.080 mg/mL for α-glucosidase compared to1.22 mg/mL of Acarbose is used as a standard. [ABSTRACT FROM AUTHOR]