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Isolavonoides represent the second largest subgroup of flavonoids and have an influence on critical molecular pathways and restore cellular homeostasis, through the reprogramming of epigenetic regulatory mechanisms. This feature indicates a crucial therapeutic potential that could be better explored to attend cancer treatment. Isoflavonoids, acting as epigenetic modulators, could contribute to the development of new therapeutic approaches in cancer, especially in onco-hematological diseases. Pterocarpans are a subgroup of isoflavonoids that have been extensively studied for their biological properties. The molecule (+)-2,3,9-trimethoxypterocarpan demonstrates high gastrointestinal (GI) absorption and the ability to cross the blood-brain barrier (BBB) in silico without violating Lipinski's rule, making it a desirable candidate in leukemia treatment. The synthesis of this molecule dates back more than a decade. In silico models, such as SwissADME, corroborate the notion of good intestinal absorption and the ability to cross the BBB. Also, it is suggested that P-glycoprotein is a substrate, which is related to its potential for active efflux from both the BBB and GI. This review highlights the biological mechanisms of this class of natural products from a translational perspective, emphasizing their chemical properties and epigenetic biological activities, which offer new therapeutic perspectives, particularly in oncology.