Two symmetry and five asymmetry mono-carbonyl analogues were synthesized with curcumin as leading compound. Their structures were characterized by IR, MS and ¹H NMR techiniques. Their antibacterial activities in vitro were tested using 11 drug-resistant strains isolated in clinical. The cytotoxicity activities in vitro were evaluated by MTT assay using 3 human cancer cell lines. Compound A5 exhibited a comparable antitumor activity with curcumin and showed high antibacterial activity. Due to the good bioactivities, single-crystal of A5 was cultured and its structure was determined using single-crystal X-ray diffraction. The crystal structure of compound A5 is orthorhombic system, space group Fdd2, with cell dimensions of a＝26.085(3) ?, b＝28.248(3) ?, c＝7.9615(9) ?, α＝90.00°, β＝90.00°, γ＝90.00°, V＝5866.4(12) ?³, Z＝16, D_X＝1.288 Mg/m³, μ＝0.09 mm^－1, F(000)＝324, The final R＝0.047, wR＝0.112.

Key words: mono-carbonyl curcumin analogue, chalcone, synthesis, anti-tumor, antibacterial activity, crystal structure