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Radiobromination of closo-dodecaborate anion. Aspects of labelling chemistry in aqueous solutions using Chloramine-T
Uppsala universitet, Medicinska och farmaceutiska vetenskapsområdet, Medicinska fakulteten, Institutionen för onkologi, radiologi och klinisk immunologi.
Uppsala universitet, Medicinska och farmaceutiska vetenskapsområdet, Medicinska fakulteten, Institutionen för onkologi, radiologi och klinisk immunologi.
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2002 (engelsk)Inngår i: Radiochimica Acta, ISSN 0033-8230, E-ISSN 2193-3405, Vol. 90, nr 4, s. 229-235Artikkel i tidsskrift (Fagfellevurdert) Published
Abstract [en]

Closo-dodecaborate dianion is a three-dimensional aromatic inorganic molecule, which can be easily halogenated forming a stable halogen-boron bond. Derivatives of closo-dodecaborate were considered as a convenient chemical form of delivery of enriched 10B to malignant tumors for boron neutron capture therapy (BNCT). Some properties of closo-dodecaborate (hydrophilicity, strength of halogen-boron bond, charge at lysosomal pH) make it attractive as a potential prosthetic group for attachment of radioactive halogens to tumor-targeting proteins. Bromine radioisotopes possess a variety of useful nuclear characteristics, and can be used in different areas of clinical diagnostics and therapy. In this work, a basic chemistry of closo-dodecaborate radiobromination was studied. It was found, that di(triethylamonium) dodecahydro-closo-dodecaborate can be labelled in high yield, more then 90%, in a wide pH range. By decreasing the pH, the bromination can be directed to closo-dodecaborate in the presence of phenolic compounds. The results of the study indicate a possibility of using the radioactive bromine label for investigation of pharmacokinetics of boronated compounds for BNCT.

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2002. Vol. 90, nr 4, s. 229-235
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URN: urn:nbn:se:uu:diva-62500OAI: oai:DiVA.org:uu-62500DiVA, id: diva2:90411
Tilgjengelig fra: 2008-06-16 Laget: 2008-06-16 Sist oppdatert: 2017-11-30bibliografisk kontrollert

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Tolmachev, VladimirLundqvist, HansSjöberg, Stefan

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