Breast cancer is the most common invasive cancer in women, and the second main cause of cancer death in women, after lung cancer. There is continuous advancement in the development of therapeutic agents against breast cancer in the recent years and still in progress. Development of hybrid molecules by combining different pharmacophores to obtain significant biological activity is an excellent approach. Coupling of coumarin scaffold with other distinct motifs has led to design of newer compounds against breast cancer. These distinct pharmacophores possess diverse mode of action as well as selectivity. It has been reported in literature that coumarin hybrids possess significant potency against breast cancer by binding to various biological targets which are associated with breast cancer. Due to low toxicity profile on various organ systems, coumarin hybrids have nowadays attracted the keen attention of researchers to explore their therapeutic ability against breast cancer. Reported coumarin hybrids include coupling with isoxazole, thiazole, monastrol, chalcone, triazole, sulphonamide, triphenylethylene, benzimidazole, pyran, imidazole, stilbene, oestrogen, phenylsulphonylfuroxan etc. In the present review, a description of various coumarin hybrid molecules has been presented along with their structural-activity relationships.