A novel series of 5-(5-substituted-1,3,4-oxadiazol-2-yl)benzene-1,2,3-triols (3n-z) was designed, synthesized, and evaluated for its potential antioxidant activities. Structural modifications at position 5 of the 1,3,4-oxadiazole scaffold (linked to a fixed antioxidant 3,4,5-trihydroxyphenyl moiety at position 2 of the ring) was expected to give new 1,3,4-oxadiazole derivatives with a wide spectrum of biological antioxidant activities. Undoubted elucidation and full confirmation of the chemical structures of all the newly synthesized compounds were accomplished using the spectroscopical and elemental analyses. The pharmacological screening for evaluation of the antioxidant activity of these new thirteen target 5-substituted-2-(3,4,5-trihydroxyphenyl)-1,3,4-oxadiazoles (3n-z) was done by using two of the most common in vitro antioxidant assays. The results of both assays showed that compounds 3w,s,u (the fumaric, malonic, and citric acids-derived 1,3,4-oxadiazoles, respectively) surprisingly exhibited very high and significant antioxidant activities, and they could be very promising lead and parent compounds for the design and synthesis of new antioxidant agents by further in vivo biological evaluations, structural modifications, and computational studies.

A series of new coumarin containing compounds were synthesized from 4-bromomethylcoumarin derivatives and different heteroaromatic systems methylene thiolinker. Twenty-four compounds were screened biologically against two human tumor cell lines, breast carcinoma MCF-7 and hepatocellular carcinoma HePG-2, at the national cancer institute, Cairo, Egypt using 5-fluorouracil as standard drug. Compounds hh and showed strong activity against both MCF-7 and HepG-2 cell lines with being compound is the most active with IC values of 5.5 µg/ml and 6.9 µg/ml respectively. Docking was performed with protein 1KE9 to study the binding mode of the designed compounds.

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