ABSTRACT: Ten (E1-E2) compounds of 1-Substituted tetra hydro pyrimidine derivatives synthesized by leuckart reaction using microwave irradiation. The structure of synthesized ten compounds were elucidated by IR, MASS, H’NMR Spectroscopy. Further these compounds were evaluated for invitro anticancer activity, antibacterial activity, and antifungal activity. Invitro antioxidant activity was carried out DPPH (Diphenylpicrylhydrazyl) method. Invitro anticancer activity (osteosarcoma) was carried out by MTT assay (3-[4, 5-dimethyl thiazol-2yl] 2, 5-diphenyl tetrazolium bromide) using human osteosarcoma cell line.  Antibacterial, Antifungal activity was carried out by disc- diffusion method, using muller-hinton agar medium and potato dextrose agar medium. All compounds, were found to have good antibacterial activity and 4 compounds (E3) 2-amino-6-[4-(dimethyl amino)phenyl]-4-oxo-1-(1-phenyl ethyl)1,4,5,6-tetra hydro pyrimidine 5-carbonitril, (E4) 2-amino -4-oxo [2-phenyl ethenyl]-1-(1-phenyl ethyl) 1,4,5,6 tetra hydro pyrimidine 5- carbonitrile, (E8) 2 amino -6-[4-( dimethyl amino) phenyl] 1-diphenyl methyl-4-oxo 1,4,5,6 tetra hydro pyrimidine -5- carbonitrile,(E9) 2 amino-1-(diphenyl methyl)-4-oxo-6-[(E)-2-phenylethenyl] 1,4,5,6-tetra hydro pyrimidine 5-carbonitrile were found to be possess antibacterial activity as compared to standard drugs.  All compounds having anticancer activity and the 2 compounds (E3 and E4) showed the potent anticancer activity with least effect on normal cells.