10-Propargyl-10-deazaaminopterin is primarily investigated for its potential in cancer therapy, particularly as an antimetabolite in the treatment of various malignancies. It functions by inhibiting key enzymes involved in folate metabolism, such as dihydrofolate reductase, which is crucial for DNA synthesis and cell proliferation. This inhibition disrupts the growth of cancer cells, making it a promising candidate for chemotherapy. Research has shown its efficacy in targeting solid tumors and hematologic cancers, often with reduced toxicity compared to traditional antifolate drugs. Additionally, it is being explored in combination therapies to enhance its anticancer effects and overcome drug resistance. Its propargyl group also offers potential for further chemical modifications, enabling the development of targeted drug delivery systems.