Synthesis of hybrid distamycin-cysteine labeled with 99mTc: a model for a novel class of cancer imaging agents |
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Authors: | Baraldi P G Romagnoli R Duatti A Bolzati C Piffanelli A Bianchi N Mischiati C Gambari R |
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Affiliation: | Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy. pgb@dns.unife.it |
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Abstract: | The synthesis of a hybrid constituted by distamycin A and cysteine labeled with the gamma-emitting radionuclide 99mTc to afford the conjugate complex 5 is reported. This new radiopharmaceutical is of potential interest as tumor imaging agent in diagnostic nuclear medicine. The preparation of the hybrid distamycin A-cysteine 4 has been achieved by coupling deformyldistamycin A and Boc-Dmt-OH. Compound 4 was then successfully labeled with 99mTc by reaction with the novel, high-electrophilic, metal-containing fragment [99mTc(N)(PP)]2+ (PP = diphosphine ligand) yielding the 1:1 complex 5. |
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