skip to main content

Title: Design of site specific radiopharmaceuticals for tumor imaging. (Parts I and II)

Part I. Synthetic methods were developed for the preparation of several iodinated benzoic acid hydrazides as labeling moieties for indirect tagging of carbonyl-containing bio-molecules and potential tumor-imaging agents. Biodistribution studies conducted in mice on the derivatives having the I-125 label ortho to a phenolic OH demonstrated a rapid in vivo deiodination. Part II. The reported high melanin binding affinity of quinoline and other heterocyclic antimalarial drugs led to the development of many analogues of such molecules as potential melanoma-imaging agents. Once such analogue iodochloroquine does exhibit high melanin binding, but has found limited clinical use due to appreciable accumulation in non-target tissues such as the adrenal cortex and inner ear. This project developed a new series of candidate melanoma imaging agents which would be easier to radio-label, could yield higher specific activity product, and which might demonstrate more favorable pharmacokinetic and dosimetric characteristics compared to iodochloroquine.
Authors:
Publication Date:
OSTI Identifier:
5817010
Resource Type:
Thesis/Dissertation
Resource Relation:
Other Information: Thesis (Ph. D.)
Publisher:
Lehigh Univ.,Bethlehem, PA
Research Org:
Lehigh Univ., Bethlehem, PA (USA)
Country of Publication:
United States
Language:
English
Subject:
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY; 62 RADIOLOGY AND NUCLEAR MEDICINE; IODINE ISOTOPES; TISSUE DISTRIBUTION; RADIOPHARMACEUTICALS; CHEMICAL PREPARATION; BRAIN; MICE; NEOPLASMS; RADIOISOTOPE SCANNING; ANIMALS; BODY; CENTRAL NERVOUS SYSTEM; COUNTING TECHNIQUES; DISEASES; DISTRIBUTION; DRUGS; ISOTOPES; LABELLED COMPOUNDS; MAMMALS; NERVOUS SYSTEM; ORGANS; RODENTS; SYNTHESIS; VERTEBRATES 400702* -- Radiochemistry & Nuclear Chemistry-- Properties of Radioactive Materials; 550601 -- Medicine-- Unsealed Radionuclides in Diagnostics