Boron Compounds for Neutron Capture Therapy
There have been two main approaches to the development of boron compounds for neutron capture therapy (BNCT). One has involved the synthesis of boronated analogues of organic structures which possess a high degree of selectivity for neoplastic cells. These include amino acids, nucleic acid precusors, porphyrins and promazines. The second approach has emphasized the use and incorporation of boron compounds into monoclonal antibodies targeted against tumor associated antigens. There have been several important requirements in achieving the use of antibodies for BNCT. First, the conjugation of boron to monoclonal antibodies must occur with significant retention of the antibody’s immunoreactivity. Second, sufficient numbers of boron atoms have to be incorporated and at least 103 boron atoms per protein molecule is necessary if a goal of 109 boron atoms per tumor cell is to be attained. Third, separation of the boron-containing antibody from the unconjugated species and from the boron entity used in the conjugation is essential. Finally, the boron-loaded antibody must have the ability for targeting all the tumor cells, under in vivo conditions with a high degree of selectivity. Research at The Ohio State University on the incorporation of boron-containing polymers into monoclonal antibodies has already been described1. The work presented herein outlines the synthesis of boronated analogues of promazines and phthalocyanines, structures which have a demonstrated proclivity for certain neoplasms. The tissue distribution data in tumor-bearing animals for certain of these compounds are presented.
KeywordsBoron Atom Tumor Associate Antigen Nitrogen Mustard Include Amino Acid Boron Compound
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