Plants have been utilized for health and medicinal benefits for hundreds of years due to their multiple beneficial attributes such as anticancer, antitumor, antioxidant, antimicrobial, antibacterial, anti-ulcer, anti-arthritic, etc. It has been estimated that there are altogether 250,000 species of higher plants on Earth and among them 35,000–70,000 species are being used to treat various diseases due to the presence of secondary metabolites (alkaloids, flavonoids, steroids, glycosides, saponins, etc.). Cancer is a worldwide leading cause of morbidity and mortality. To cure this at right time, herbal drugs are more beneficial than synthetic drugs, because the synthetic medicines can cause heavy damage to normal cells while destroying the tumor cells. The present work consists of a review of 149 plant families harboring 667 species reported to possess anticancer property. Moreover, other biological properties of the bioactive compounds are also covered. This work is based on reliable data collected from multifarious databases such as CAB abstract, MEDLINE, EMBASE, J GATE, ERIC, Proquest, INMEDPLAN, NATTS, The Plant List, JSTOR, Google Scholar, Springer, Elsevier, and websites such as www.sciencedirect.com, www.jstor.org, www.eflora.org, and www.pfaf.org. The complete data regarding plant names, synonyms, common names, botanical description, medicinal properties, and bioactive compounds present in the plant parts is compiled. In near future, these bioactive compounds can be deployed singly or in combination with routine chemotherapy and radiotherapy to treat various types of cancers, after proper standardization, dose optimization, and stringent clinical trials.