During the last 2 decades, the study of the biological activities of Coumarin derivatives has been the aim of many researchers. Based on these findings, a series of Coumarin substituted benzothiazoles were synthesized by refluxing Coumarin-4-carboxaldehyde and oaminothiophenol in acetic acid. Compounds were characterized by IR, 1H NMR and mass spectroscopy. All the compounds were tested for their anticancer activity against MCF-7 breast cancer cell line with MTT assay. Most of the compounds showed moderate to good anti-breast cancer activity. Docking studies of the synthesized compounds was done with the help of VLife MDS 3.0 software using GRIP batch docking method to study their observed activity.