Hematological malignancies for a very large percentage of cancers occurring the world over and lead to a very large number of deaths each year. It is not just the disease but also the currently available cure which are equally responsible for the side effects and discomfort experienced by the patients. The side effects of the current chemotherapeutic agents' available range from mouth ulcers, diarrhea, temporary hair loss, rashes, nausea, vomiting, and fatigue to low blood cell counts, increased risk of infections, graft versus host disease, tumor lysis syndrome, differentiation syndrome, and difficulty in conceiving. Due to these myriad side effects researchers and on a continuous lookout for newer treatment alternatives. For most developing countries one of the most attractive options is offered by herbals or plant-based medicines. One such herb is Cyclea peltata. It is a climbing shrub found aplenty in southern and eastern India. It has been used traditionally to cure lots of minor ailments. This paper explores the possibility of using the root extract for the treatment of leukemia. To do this, the extracts of the roots were prepared in different organic solvents to ensure complete extraction of all phytoconstituents fractions. The extracts were then tested on 3 different human cell lines. The potential cause of the antileukemic potential of the plant was also hypothesized and proven by carrying out antioxidant studies using the DPPH free radical scavenging assay. The probable active constituents were identified using the liquid chromatography-mass spectrometry assessment, wherein the responsible fractions were successfully identified. The studies showed that the alkaloid and phenolic phytoconstituents were responsible for the antileukemic potential via their antioxidant activity. This lays down the groundwork of offering a new and safer treatment option that could be further explored to be made into one having actual clinical outreach.