Antibody-directed enzyme prodrug therapy (ADEPT) has potential as an effective and highly specific modality of treatment for many different cancers, especially those that are difficult to target such as glioblastoma multiforme (GBM)1. By utilizing ADEPT in conjunction with a prodrug-derived anticancer agent, GBM cells can be destroyed while limiting damage to the surrounding healthy tissue. Tumor-associated macrophages that surround GBM cells are targets for the antibody-enzyme conjugate, followed by activation of the prodrug within the vicinity of the catalytic enzyme. Methotrexate (MTX) is an inhibitor of dihydrofolate reductase and is therefore a potent prodrug candidate for the treatment of GBM.<br/><br/>In this poster, we are presenting our recent efforts towards the completion of the synthesis of the prodrug form MTX-α-3-cyclopentylphenylalanine. While most synthetic steps have been successful, the 3-cylcopentyl phenylalanine derivative has proven difficult to synthesize. Several alternative routes will be presented.<br/>

Progress on the synthesis of a methotraxate-phenylalanine derivative for the treatment of glioblastoma in antibody-directed enzyme prodrug therapy

253rd National Meeting (2017)

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