Garlic (Allium Sativum ) and its therapeutic effects in prevention and treatment of various diseases has been recognized by several different cultures throughout the history. Of numerous health benefits of garlic, recent studies support its protective effect against different types of cancer risk and a potential inhibition of several pathogens. The anti-tumor and anti-microbial agent present in garlic are widely being recognized for their targets to be used as a potential therapeutics. This review summarizes the molecular mechanism of different garlic compounds and their targets in cancer and antipathogenic activity.