Abstract
The successful use of p-boronophenylalanine (BPA) as the agent for the delivery of boron to melanoma for NCT is based on it being incorporated with tyrosine as a precursor for melanin synthesis. 1 Ideally for the patient undergoing NCT, the boron concentration in the tumour should reach 20 to 30 ppm, and for BPA this level can be achieved by the administration of very high doses. However, the procedure would be improved by a compound with the same affinity for the tumour but with a larger boron content. Consequently a new generation of boronated amino acids are being synthesised to take advantage of the unique bonding characteristics of boron and its ability to form cluster compounds containing up to 12 boron atoms in a compact structure. Following this approach, we have synthesised a 1,2-dicarba-closo-dodecaboranyl derivative of phenylalanine and its nido analogue.
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Prashar, J.K., Moore, D.E., Wilson, J.G., Allen, B.J. (1993). Synthesis of Carboranylphenylalanine for Potential Use in Neutron Capture Therapy. In: Soloway, A.H., Barth, R.F., Carpenter, D.E. (eds) Advances in Neutron Capture Therapy. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-2978-1_54
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DOI: https://doi.org/10.1007/978-1-4615-2978-1_54
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