Cancer is a terrifying disease that has become one of the world’s most challenging health concerns, necessitating a proactive approach to its treatment. Nature is a rich source of new chemical entities and a promising avenue for cancer research. Because of their different modes of action on target events in many ways, nature-derived chemicals are considered good possibilities for anticancer drug development. The current review article highlights recent breakthroughs in cancer therapeutics, including natural therapeutic molecules and their mechanisms of action against cancer treatment, as well as their limits, challenges, and prospect. For the review, article data have been collected from previously studied and published research reports, clinical evaluations, case studies, and clinical statistical data generated by scientific research organizations of repute. The chemical structures have been drawn using computational software (chemsketch). The development of promising candidates that can prevent or reduce the proliferation of cancer cells without causing adverse effects from these therapeutics is now underway. Further, nature-derived products are a game-changer because they are simple, safer, environmentally friendly, low-cost, quick, and less toxic than traditional treatment techniques. However, many bioactive chemicals and their analogs have been discovered as possible anticancer treatment options. In the review, the potent therapeutics phytochemicals derived from nature with their tremendous anticancer effects with limitations and prospects have been studied and analyzed based on previously published articles and reports.