Coumarin 7 exhibits a broad spectrum of bioactivities with notable antiproliferative, enzymatic, and antiviral properties. It demonstrates antiproliferative efficacy on a range of cell lines such as human U87 MG, mouse B16, human SiHa, mouse NIH3T3, and HUVEC with IC50 values ranging from 9300.0 nM to 15000.0 nM, but shows lower efficacy on human HeLa and DLD1 cell lines with IC50 values greater than 70000.0 nM. The compound also inhibits luciferase enzymes including Photinus pyralis and Renilla reniformis, achieving complete inhibition of Photinus pyralis luciferase at 0.04 µM. Additionally, it targets ubiquitin-specific proteases, Menin-MLL interaction, Lamin A splicing, BRCT-phosphoprotein interactions, Caspases, and is involved in key biochemical and cellular processes like miRNA modulation, genomic imprint erasure, hemoglobin beta chain splicing, and DNA repair inhibition.
In terms of antiviral activity, Coumarin 7 is effective against X4 tropic HIV-1 clone pNL4-3 in H9 cells with an IC50 of 240.0 nM and shows low cytotoxicity with a CC50 greater than 50,000.0 nM. It also inhibits the Vif/human APOBEC3G complex with a significant fold change compared to control. Against SARS-CoV-2, the compound inhibited the 3CL-Pro protease by 22.09% at 20µM and reduced virus-induced cytotoxicity in VERO-E6 cells with an IC50 value of 360.0 nM and a high selectivity index of 91.67. Additionally, it inhibited SARS-CoV-2-induced cytopathy in EGFP-labeled monkey Vero cells with an IC50 value of 0.3531 µM. This demonstrates Coumarin 7's potent antiviral potential, along with a favorable therapeutic index..
Note: Summary generated by AI. Data source: ChEMBL 