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AbstractAbstract
[en] The antitumor antibiotics bleomycins labeled with 57Co are known to possess excellent tumor localizing properties but the rather long halflife of 57Co prevents its use in clinical routine. It is therefore desirable to label cobalt-bleomycin with a more suitable radionuclide, e.g. 123I. This thesis reports on further studies on cobalt-bleomycin. It appears from the studies on the structure of cobalt-bleomycin described in this thesis (Chapter B), that cobalt is able to form different complexes with bleomycin (the forms I and II). The difference in structure is not clear, but the biological behavior of both forms is studied (Chapter C). In Chapter D the iodination of cobalt-bleomycin is described. Iodination of free bleomycin yields a product with bad tumor localizing properties, and straight-on iodination of cobalt-bleomycin is prevented by the presence of cobalt. To retain the good tumor-localizing properties of cobalt-bleomycin, possibilities were explored to incorporate the iodine in the terminal amine (a side chain, not involved in complexation). Alkylation of cobalt-bleomycin demethyl A2 with N-bromoacetyl-3-iodoaniline yielded a product; unfortunately this product possessed bad tumor localizing properties and moreover, was not stable in vivo. The structure of a possibly successful iodinated cobalt-bleomycin is outlined but could not be realized during this research. (Auth.)
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Source
8 Jan 1982; 150 p; Includes Dutch summary; 194 refs.; Proefschrift (Dr.).
Record Type
Miscellaneous
Literature Type
Thesis/Dissertation
Report Number
Country of publication
ANTIBIOTICS, ANTIMITOTIC DRUGS, BETA DECAY RADIOISOTOPES, CHEMICAL REACTIONS, COMPLEXES, DAYS LIVING RADIOISOTOPES, DISEASES, DRUGS, ELECTRON CAPTURE RADIOISOTOPES, HALOGENATION, INTERMEDIATE MASS NUCLEI, IODINE ISOTOPES, ISOTOPE APPLICATIONS, ISOTOPES, KINETICS, MEDICINE, NUCLEI, ODD-EVEN NUCLEI, ORGANIC COMPOUNDS, RADIOISOTOPES, REACTION KINETICS, TRANSITION ELEMENT COMPLEXES
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