SARS-CoV-2-IN-29 is a two-armed diphosphate ester with benzene system and molecular tweezers. SARS-CoV-2-IN-29 exhibits antiviral activity with IC 50 s of 1.5 μM and 1.6 μM against SARS-CoV-2 activity and the spike pseudoparticle transduction, respectively. SARS-CoV-2-IN-29 induces liposomal membrane disruption with an EC 50 value of 3.0 μM.