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Title: New [sup 99m]Tc, [sup 186]Re, and [sup 109]Pd complexes of SN and PN ligand systems

Miscellaneous ·
OSTI ID:7165654

The development of new site specific radioisotope tracers which would permit quantitative in vitro and in vivo studies of physiological and biochemical processes continues to be an essential aspect in the design of new radiopharmaceuticals for diagnostic and therapeutic applications. In carrying out this objective, a new class of ligand frameworks based on the conventional amine thiol ligands and the unconventional PN ligand systems were designed for use in labeling proteins and monoclonal antibodies with both gamma and beta emitting isotopes for potential use as radioimmunodiagnostic and radioimmunotherapeutic agents respectively. Systematic synthetic investigation involved the development of new N[sub 3]S[sub 2] and main group PN ligands and their chemical tuning to achieve optimal in vitro and in vivo stability characteristics of the resulting metal chelates. The fundamental coordination chemistry of these ligands with different transition metals (e.g., Pd, Re) was developed to gain insight into their reactivity with both early and late transition metal radionuclides. Detailed characterization of these ligands and their metal complexes were undertaken via various analytical, spectroscopic and extensive X-ray crystallographic techniques. The ligands were labeled with [sup 99m]Tc, [sup 186]Re and [sup 109]Pd and their complexation yields determined. The radiochelates were analyzed for their radiochemical purity and in vitro stability and characterized by various radiochemical techniques. The new bifunctional chelating agents were used to label human IgG with [sup 99m]Tc. The conjugation yields and the in vitro stabilities of these radiolabeled proteins were examined. The results of these studies demonstrate the potential utility of using a wide spectrum of S-N and P-N based ligands to produce a new genre of complexes for the development of future radiopharmaceuticals and bioconjugates.

Research Organization:
Missouri Univ., Columbia, MO (United States)
OSTI ID:
7165654
Resource Relation:
Other Information: Thesis (Ph.D.)
Country of Publication:
United States
Language:
English