The concept that bioactive components in functional foods are efficacious for the improvement of health, has recently gained much importance. The cruciferous vegetables which include broccoli, cabbage and cauliflower are excellent source of phytochemicals including glucosinolates and their byproducts, phenolics and antioxidant vitamins as well as dietary minerals. Broccoli consumption mediates a variety of functions including providing antioxidants, regulating enzymes and controlling apoptosis and cell cycle. The organosulfur chemicals namely glucosinolates and the S-methyl cysteine sulphoxide found in broccoli in concert with other constituents such as vitamins E, C, K and the minerals such as iron, zinc, selenium and the polyphenols namely kaempferol, quercetin glucosides and isorhamnetin are presumably responsible for various health benefits of broccoli. There exists no comprehensive review on the health promoting effects of phytochemical compounds present in broccoli so far. This review compiles the evidence for the beneficial role of glucosinolates in conjugation with the other phytoconstituents for human health. It also gives an overview on the chemical and biological characterization of potential bioactive compounds of broccoli including the interaction of phytoconstituents on its bioactivity. Further, the molecular basis of the biological activities of the chemicals present in broccoli potentially responsible for health promotion, from chemoprevention to cardio protection, are outlined based on in vitro and in vivo studies with a note on the structure activity relationship of sulforaphane and a few other isothiocyanates.