In this work, the multifunctional potential of four 3-acetylcoumarin derivatives was studied. The derivatives were significantly active against bacteria Staphylococcus aureus, Pseudomonas aeoginosa and fungal strain Candida albicans. The results of antioxidant activity assays were promising when compared to ascorbic acid. The in vitro anticancer activity was carried out using MTT assay on human cancer cell line COLO-205 and 3ACDT showed commendable antiproliferative activity along with appreciable tumor selectivity with distinct selectivity index. Moreover, ADMET properties of the compounds were determined using the pKCSM and SwissADME online tools and all compounds were found with good pharmacokinetic profile. Hence, from the obtained results from all the 3-acetylcoumarin derivatives, 3ACDT exhibited good therapeutical potential and can be optimized for lead development.