The synthesis of a hybrid constituted by distamycin A and cysteine labeled with the ?-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.

Synthesis of hybrid distamycin-cysteine labeled with Tc-99m: a model for a novel class of cancer imaging agents

Bolzati C;
2000

Abstract

The synthesis of a hybrid constituted by distamycin A and cysteine labeled with the ?-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.
2000
Cysteine
Distamycins
Humans
Neoplasms
Organotechnetium Co
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.14243/123732
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