Objective: The objective of the present study is to evaluate the anticancer potential of lovastatin obtained from fungal source.Methods: About 15 fungal cultures were isolated from soil samples collected from Bharathiar University, India, and all are identified and characterized through microscopic characterization. Lovastatin producing capability was confirmed through bioassay against Saccharomyces cerevisiae, and the ability of selected fungus to produce lovastatin was further confirmed by high-performance liquid chromatography. Maximum lovastatin producing fungi were further selected for purification (overloaded elution chromatography) and characterization done using inhibition rate (IR). 5-diphenyl tetrazolium bromide (MTT) assay using A549 cell line was performed for antitumor activity evaluation.Results: Among the 15 isolates, Aspergillus flavus exhibited the maximum zone of inhibition (1.5 cm) against the test organism through solid-state fermentation. The resemblance in retention time (RT) of peak shown in chromatograms of standard lovastatin (RT=25.1 minutes) and sample (RT=25.1 minutes) were similar. This confirmed the presence of lovastatin in the selected fungal isolate (A. flavus). The presence of two functional groups in lovastatin C=O and O-H was confirmed by IR spectrum 50% of cell lysis was observed in MTT assay.Conclusion: Lovastatin obtained from soil fungi is capable of producing lovastatin in good proportions. Obtained fungal lovastatin exhibited significant antitumor activity against A549 cell line. Like other biological derivatives, lovastatin from soil fungi had greater potential in anticancer activity, and further biosynthetic pathway insights in their production can improve the yield which aid in large scale production.