A Potential New BNCT Agent
Boron neutron capture therapy (BNCT) is a binary approach to cancer therapy.1 In this protocol, boron-10 is delivered to the tumor tissue, and upon irradiation with thermal neutrons, cytotoxic α-particles and high energy lithium-7 ions are produced. The linear energy transfer (LET) of these heavy charged particles (which is on the order of one cell diameter) makes them lethal to the boron-containing cells. The success of this protocol is dependent upon the selective delivery of a sufficient quantity of boron-10 to the tumor tissues (10–30μg boron-10/g of tumor with tumor to normal tissue ratio of 3:1). While various carrier molecules are under investigation as potential boron-delivery agents, the only drug currently in clinical trials in the United States is a boron-containing amino acid,2 4-dihydroxyborylphenylalanine (BPA).
KeywordsLinear Energy Transfer Boron Neutron Capture Therapy Pressure Tube Potassium Cyanide Dynamic Positron Emission Tomography
Unable to display preview. Download preview PDF.
- 2.J.A. Coderre, E.H. Elowitz, M. Chadha, R. Bergtland, J. Capala, D.D. Joel, H.B. Liu, D.N. Slatkin, and A.D. Chanana, Boron Neutron Capture Therapy for Glioblastoma Multiforme Using p-Boronopheny- lalanine and Epithermal Neutrons: Trial Design and Early Clinical Results, J. Neurooncol. 33:141, 1997.PubMedCrossRefGoogle Scholar
- 3.K.F. Hubner, G.T. Smith, J.A. Thie, and E. Buonocore, Dynamic Positron Emission Tomography (PET) of Brain Tumors Using l-Aminocyclobutane[C-ll]carboxylic Acid (C-ll ACBC) and A 2-Component Model, J. Nucl. Med., 33:922, 1992.Google Scholar
- 4.R.N. Grimes, “Carborane,” Academic Press, New York and London, 1970.Google Scholar
- 5.R.R. Srivastava, R.R. Singhaus, and G.W. Kabalka, Synthesis of l-Amino-3[2-(l,7-dicarba-closo-dode-caboran(12)-l-yl)ethyl]cyclobutanecarboxylic Acid: A Potential BNCT Agent, J. Org. Chem., 62:4477, 1997.Google Scholar
- 9.H.R. Henze, and R.J. Speer, Identification of Carbonyl Compounds through Conversion into Hydantoins, J. Org. Chem., 2:1316, 1942.Google Scholar
- 10.Analytical data of galactose-containing meta-carboranyl ACBC 3: 1H NMR (CD3OD) δ 4.35 (d, J = 5.80Hz, 1H), 4.00-3.40 (m, 4H), 2.66 (m, 2H), 2.42 (m, 3H), 2.20-1.75 (m, 4H), 1.61 (m, 2H). 13C NMR (CD3OD) δ 176.64, 98.18 (94.06), 77.35, 75.30, 74.96 (75.11), 74.84 (71.07), 73.62 (70.25), 72.97 (70.17), 55.91 (58.20), 40.09, 37.66 (38.47), 36.02(36.69), 35.33(35.80), 29.07 (28.85). Anal. Calcd. for C15H34BC1N07: C, 37.22; H, 7.08; N, 2.89. Found: C, 36.97; H, 7.05; N, 2.67.Google Scholar