Radioiodination and biodistribution of analogs of a calichemicin constituent.
Analogs of the aromatic constituent of calichemicins were labeled with 131I by exchange reactions. Radiochemical yield for methyl-4-hydroxy-5-iodo-2,3-dimethoxy-6-methylbenzoate was approx. 90%. For methyl-4-benzyloxy-2-hydroxy-3-iodo-6-methylbenzoate the yield was about 30%. Biodistribution studies were carried out in mice following intravenous administration of tracer doses. Average brain uptake of the first compound at 3 min was 0.28%, and that of the second 1.96%. Tissue distribution of the two compounds elsewhere was similar in nature. High uptake was observed initially in the liver; this reduced with time, while radioactivity in the GI-tract increased. The benzylated compound appeared potentially useful for designing a brain imaging radiopharmaceutical.
Department of Nuclear Medicine, University of Connecticut Health Center, Farmington 06060.
H B
HB
Patel
F
F
Hosain
R P
RP
Spencer
H D
HD
Scharf
M S
MS
Skulski
A
A
Jansujwicz
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000493:pharmacokinetics*; D007457:Iodine Radioisotopes; D007553:Isotope Labeling; D051379:Mice; D010226:Parabens / Q000493:pharmacokinetics; D012459:Salicylates / Q000493:pharmacokinetics; D014018:Tissue Distribution
D000903:Antibiotics, Antineoplastic; D007457:Iodine Radioisotopes; D010226:Parabens; D012459:Salicylates; C071348:methyl 4-benzyloxy-2-hydroxy-3-iodo-6-methylbenzoate; C071347:methyl 4-hydroxy-5-iodo-2,3-dimethoxy-6-methylbenzoate