Synthesis of 4'-epi-iodo-4'-deoxy-daunorubicin, a potential cancer radiotherapeutic agent.
We have prepared 4'-epi-iodo-4'-deoxy-daunorubicin (IDDNR)(1), a doxorubicin analog, via a 5-step synthesis involving a protected daunorubicin triflate derivative (4). This triflate derivative will allow the facile and regiospecific nucleophilic preparation of I-125 or Br-80 m labelled analogs of IDDNR. Auger electron-emitting I-125- or Br-80 m-labelled analogs of IDDNR may have potential as cancer radiotherapeutic agents.
Murali
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Dept. of Medical Physics, University of Wisconsin Medical School, Madison 53706, USA.
DeJesus
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D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis*; D003630:Daunorubicin / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D007364:Intercalating Agents / Q000138:chemical synthesis*; D007457:Iodine Radioisotopes / Q000627:therapeutic use*; D009369:Neoplasms / Q000532:radiotherapy*
D000903:Antibiotics, Antineoplastic; D007364:Intercalating Agents; D007457:Iodine Radioisotopes; C041984:4'-deoxydaunomycin; D003630:Daunorubicin