One of the primary health issues affecting people and having the highest fatality rate is cancer. The agents that cause cancer can be biological, synthetic, or chemical. It is treated with a variety of medications, but they all have harmful side effects. As a result, extensive research is being done to create new, efficient, and cost-effective anticancer medications with greater selectivity, smaller dosages, and less side effects. Due to their enormous success rate in creating active pharmaceutical intermediates, heterocyclic chemistry has received increased attention in drug discovery throughout the years. One of the most significant heterocyclic compounds with outstanding pharmacological properties is benzoxazole, which belongs to the class of heterocyclic compounds. There have been several reports of both synthetic and naturally occurring substances having a very strong anti-cancer action in the benzoxazole backbone. Designing benzoxazole-containing compounds, synthesising them, and gathering data on their anticancer effectiveness against diverse human cancer cell lines have all advanced significantly in various research groups. The anticancer activity of diverse benzoxazole compounds synthesised by different groups has been examined in an effort to determine how varied heterocyclic moiety coupled with benzoxazole have an effect on it. A summary of all these recent articles aids in pointing the way for additional research.