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In the present study, a novel phosphoramide (L) and corresponding phosphoramide-functionalized graphene oxide (GO-L) were synthesized. L was characterized by FT-IR, ¹H NMR, ¹³C NMR, ³¹P NMR, and Mass spectroscopy. Functionalization of L on graphene oxide (GO) was investigated by XRD, FT-IR, SEM, EDX, and Map analyses. The cytotoxic effect of L and GO-L against the MCF-7 cell line was assessed by MTT, and flow cytometry (FCM) assay. The cell viability of L and GO-L at different concentrations (0.5–200 μg. mL⁻¹) was investigated at 24 h experiment. The antitumor effect of L was improved after attachment on GO, and minimum inhibition concentration (IC₅₀) of GO-L was obtained 23.11 μg. mL⁻¹. The antimicrobial activity of the synthesized compounds was evaluated against two strains of gram-positive (Staphylococcus aureus) and gram-negative (Escherichia coli) bacteria using the disk …