Coumarin glycosides have shown immense potential for diverse biological activities and have been explored extensively as highly prospective biomolecules. In recent years, coumarin glycosides have been used as enzyme inhibitor molecules, environmentally- sensitive fluorescent sensors, the building material of single-excitation and dual emission graphene composite, fluorophore-tagged glycosides, molecule to assay enzyme activity on model bacterial strains, the nucleoside monomer unit for the photoswitchable formation of a DNA interstrand cross-link along with many other applications. In this review, we have compiled biochemically afforded coumarin glycosides obtained via mutagenic synthesis, chemo-enzymatic synthesis and hairy root culture system synthesis. This review will play the role of a reservoir of biochemically synthesized glycosylated coumarins and encourage medicinal chemists to explore the potential of these molecules as drug candidates and further biological applications.