Increasing recurrence of mammalian tumors and severe side-effects of chemotherapeutic agents reduce the clinical efficacy of a large variety of anticancer agents that are currently being used. Thus, there is always a constant need to develop alternative or synergistic anticancer drugs with minimal side-effects. One important strategy to develop effective anticancer agents is to study into anticancer agents derived from natural sources. Anticancer agents derived from plants and their derivatives have been proven to be effective for cancer prevention and therapeutics. Vinca alkaloid and their derivatives, alone and in combination with therapeutic agents, have been used for a long time for the treatment of various types of cancers. Polyphenols form one of the most important and extensively used classes of plant-derived therapeutics for cancer prevention or chemotherapy. The present review highlights a plethora of studies focused on the antineoplastic properties of plant-derived chemicals, such as Vinca alkaloid, saponins, and flavonoids.