Mithramycin (1 ) and Etoposide (2 , Fig 1) are very well known chemotherapy for years. Mithramycin (plicamycin) is an anti-neoplastic antibiotic. It inhibits RNA synthesis and is used in testicular tumor, disseminated neoplasms and hypercalcaemia. Etoposide is an inhibitor of the enzyme topoisomerase II. It is used as chemotherapy for diseases such as Ewing's sarcoma, lung cancer, testicular cancer, lymphoma, non-lymphocytic leukemia, and glioblastoma multiform. Mithramycin and Etoposide were used as warhead for our proprietary Small Molecule Drug Conjugate (SMDC) technology. Folate conjugates of these drugs were synthesized which are directed to the cancerous cells with over-expressed folate receptors. Herein we report the efficient regio-selective synthesis of folate conjugates via direct activation of the phenolic hydroxyl group of Mithramycin and Etoposide.  No additional protection of other hydroxyl groups, presented in the drug molecules, was required.  

<i>Regio</i>-selective activation of mithramycin and etoposide for synthesis of their folate conjugates

244th National Meeting (2012)

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Regio-selective activation of mithramycin and etoposide for synthesis of their folate conjugates