Cancer is the world's second leading cause of death after cardiovascular disease. Medicinal plants are important natural sources of herbs that have been used to treat various human inflammations since ancient times. Some of the bioactive molecules that lead the anticancer potentials include vinblastine, alkaloid vinca, taxan, vincristine, and camptothecin that are being used worldwide as therapeutic agents. Several studies have provided the role of medicinal plants and their association with traditional medicine systems. They have shown healing assets and effectiveness against brain and uterine tumors, lung cancer, breast cancer, blood cancer, and many more. These plants are obtained from the forest and elsewhere. Further, with a comprehensive understanding of molecular science, sophistication in isolation, and structural elucidation techniques, many anticancer plants, and their constituents, have been recognized for cancer cure. Based on the currently available literature, this chapter highlights the clinical and traditional studies exploring the anticancer potential of plants in the treatment/prevention of cancer diseases. Additionally, this chapter discusses the role of some effective antitumor-active herbal agents for cancer therapy. © The Author(s), under exclusive license to Springer Nature Switzerland AG 2021. All rights reserved.