Background: Coumarins (2H-l-benzopyran-2-ones, 2) are secondary metabolites synthesized by plants having a place with families like leguminosae, rutaceae, umbelliferae, and compositae. There is a lot of confusion with respect to the specific role of coumarins in plants yet it is referred to that they function as growth regulators, seed dormancy regulators, bacteriostats, fungistats, and so forth. Objective: The present review discusses the important biological activities of Linear pyranocoumarins having 2,2-dimethylpyran ring fused to parent coumarin structure. Methods: This review is based on a literature search done between January 2001 and August 2020 through PubMed® and ScienceDirect databases. The collected studies are both in vitro and in vivo in nature. Result: It has been found that linearly fused pyranocoumarins have numerous significant biological activities like anti-bacterial, anti-fungal, anti-cancer (activities against lung, breast, skin, prostrate cancer, leukemia, etc.), hepatoprotective activity, anti-HIV, neuroprotective activities, etc. Some research points out the presence of 2,2,-dimethylpyran ring and functional groups present on it to be the cause of such diverse biological activities. Conclusion: Thus the goal of this review is to provide knowledge as well as probing of a few of the linear pyrano coumarins which may serve as new leads for the discovery of the anti-cancer drug, anti-fungal agent, and anti-tumor promoter.