Boron neutron capture therapy using

Yanagie, H., Fujii, Y, Takahashi, T. et al. 1989. Boron neutron capture therapy using B entrapped anti-CEA immunoUposome. Human Cell 2 290-6. 

Various borate esters are chemostetilants for house flies (51). Tributyl borate, available from Eagle-Picher, Miami, Oklahoma, which is isotopically enriched in boron-10, is being used as a chemical precursor in the synthesis of pharmacologically active boron compounds suitable for boron neutron capture therapy. 

To date, the most extensively studied polyboron hydride compounds in BNCT research have been the icosahedral mercaptoborane derivatives Na2[B22H22SH] and Na [(B22H22S)2], which have been used in human trials with some, albeit limited, success. New generations of tumor-localizing boronated compounds are being developed. The dose-selectivity problem of BNCT has been approached using boron hydride compounds in combination with a variety of deUvery vehicles including boronated polyclonal and monoclonal antibodies, porphyrins, amino acids, nucleotides, carbohydrates, and hposomes. Boron neutron capture therapy has been the subject of recent reviews (254). 

Several kinds of cancer therapy use radiation to destroy malignant cells. Boron neutron capture therapy is unusual in that boron-10, the isotope injected, is not radioactive. However, when boron-10 is bombarded with neutrons, it gives off highly destructive a particles. In boron neutron capture therapy, the boron-10 is incorporated into a compound that is preferentially absorbed by tumors. The patient is then exposed to brief periods of neutron bombardment. As soon as the bombardment ceases, the boron-10 stops generating a particles. 

Sessler, J. L. Allen, W. E. Krai, V. A. Preparation of highly boronated derivatives of expanded porphyrins (texaphyrins) for potential use in boron neutron capture therapy and related applications. US Patent 5,955,586, 1999 Chem. Abstr. 1999, 131, 222611. 

Like PAMAM dendrimers, polylysine dendrimers are largely characterised by amide bonds. They attracted interest as potential therapeutic agents for use in boron neutron capture therapy and in magnetic resonance imaging (MRI) (see Chapter 8), since dendritic polylysines apparently have a lower toxicity than their linear counterparts. The polylysine shown in Fig. 4.10 with a total of 80 terminal boron atoms in the carborane units and a dansyl group was designed specifically for boron neutron capture therapy [20]. 

The dual-mechanism of cytotoxic activity of amine-boranes, possessing significant antineoplastic activity and useful also in boron neutron capture therapy (BNCT), initiated the search during recent years for therapeutic compounds of this class which accumulate preferentially in the tumor tissue194,195. The title compound 192, one of the... 

In work that also involves the use of a Mn(III) porphyrin, Huang et al. published a report on the manganese chelate of the tetrakiscarborane carboxylate ester of 2,4-(a, P-dihydroxylethyl)deuteroporphyrin IX (MnBOPP, 9, Figure 2) [19]. The free-base form of this derivative, BOPP, has demonstrated potential as an agent for boron neutron capture therapy (BNCT) [75,76] and photodynamic therapy (PDT) [77] and is known to localize selectively in cerebral glioma tumors at ratios as high as 400 1 relative to normal brain tissue [19,78]. Like the free-base, MnBOPP also selectively localizes in tumor tissue. Specifically, it has been shown to enhance preferentially the... 

Kane, R.R. Drechsel, K. Hawthorne, M.F. Automated synthesis of carborane-derived homogeneous oligophosphates Reagents for use in the immunoprotein-mediated boron neutron capture therapy (BNCT) of cancer. J. Am. Chem. Soc., 115, 8853-8854, 1993. 

The functional derivatives prepared can be used not only for boron neutron capture therapy, but also as linkers for attachment of radioactive halogen labels to biomolecules for purposes of nuclear medicine8. 

Boron cluster compounds have many electron deficient sites in them and they possess polyhedral skeleton. The procedure by which the boron cluster compounds are built from small polyhedral skeletons to a big polyhedral skeleton is in wide use for the synthesis of boron neutron capture therapy. The reactivity and reaction mechanism for the formation of the boron cluster compounds from a small cluster to a big cluster have been studied. 

Boron has two stable isotopes, (80.4% abundance) and °B (19.6%). B has a very high neutron absorption cross section (it is a good absorber of neutrons). This property has been developed for use in the treatment of cancerous tumors in a process called boron neutron capture therapy (BNCT). Boron-containing compounds having a... 

A new series of 5-carboranyl-substituted-2 -deoxyuridine (25a) and deoxy-thymidine (25b) derivatives containing a range of alkyl spacers has been prepared to access a more effective use of boron neutron capture therapy. Evaluation of these derivatives as substrates for the human thymidine kinases TKl and TK2 showed that a decrease in the length of the spacer (from 8 methylene units to 4) between the carborane moiety and the pyrimidine base resulted in better substrate characteristics. 

Svantesson E, Capala J, Markides KE, Pettersson J. Determination of boron-containing compounds in urme and blood plasma from boron neutron capture therapy patients. The importance of using coupled techniques. Anal Chem 2002 74 5358-63. 

Investigational pharmaceutical techniques also have been observed using ICP spectroscopic techniques. Boron neutron capture therapy is such an example, where malignant cells can be preferentially loaded with 10B and irradiated with thermal neutrons, thus killing the cancerous cells (59). This can be especially... 

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