Synthesis and Biological Behavior of a Boronated Analogue of the Antiestrogen U 23,469-M

1991 ◽  
Vol 46 (3-4) ◽  
pp. 252-256 ◽  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Thermal Neutron ◽  
Therapeutic Effect ◽  
Neutron Capture ◽  
Biological Behavior ◽  
Neutron Capture Therapy ◽  
Thermal Neutron Irradiation ◽  
Estrogen Receptor Positive ◽  
Specific Uptake

A boronated analogue of the antiestrogen U 23,469-M (D. Lednicer, D. W. Emmert, S. C. Lyster, and G. W. Duncan, J. Med. Chem . 12, 881 (1969)) was prepared, for possible use in neutron capture therapy of estrogen receptor-positive tumors. In this analogue, the terminal OH group was replaced by a B-decachloro-o-carboranyl residue. This com pound showed a large, non-specific uptake in ZR75-1 breast cancer-derived cells. It could partially inhibit the uptake of estradiol in these cells. Accumulation in the cells at physiologically obtainable concentrations was, however, too low to envisage a therapeutic effect following thermal neutron irradiation.

scholarly journals Monte Carlo assessment of boron neutron capture therapy for the treatment of breast cancer

2005 ◽  
Vol 20 (1) ◽  
pp. 27-32 ◽  
Author(s):  
Daniel Mundy ◽  
Tatjana Jevremovic
Keyword(s):  
Breast Cancer ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Boron Concentration ◽  
Treatment Options ◽  
Neutron Capture Therapy ◽  
Boron Neutron Capture ◽  
Thermal Neutron Irradiation ◽  
Starting Point ◽  
Her 2

For a large number of women who are diagnosed with breast cancer every year the avail able treatment options are effective, though physically and mentally taxing. This work is a starting point of a study of the efficacy of boron neutron capture therapy as an alternative treatment for HER-2+ breast tumors. Using HER-2-specific monoclonal anti bodies coupled with a boron-rich oligomeric phosphate diester, it may be possible to deliver sufficient amounts of 10B to a tumor of the breast to al low for selective cell destruction via irradiation by thermal neutrons. A comprehensive computational model (MCNP) for thermal neutron irradiation of the breast is described, as well as the results of calculations made using this model, in order to determine the optimum boron concentration within the tumor for an effective boron neutron capture therapy treatment, as compared with traditional X-ray radiotherapy. The results indicate that a boron concentration of 50-60 mg per gram of tumor tissue is optimal when considering treatment times, dose distributions and skin sparing. How ever these results are based upon best-guess assumptions that must be experimentally verified.

scholarly journals Spermidinium closo-dodecaborate-encapsulating liposomes as efficient boron delivery vehicles for neutron capture therapy

2014 ◽  
Vol 50 (82) ◽  
pp. 12325-12328 ◽  
Author(s):  
Shoji Tachikawa ◽  
Tatsuro Miyoshi ◽  
Hayato Koganei ◽  
Mohamed E. El-Zaria ◽  
Clara Viñas ◽  
...  
Keyword(s):  
Thermal Neutron ◽  
Neutron Irradiation ◽  
Neutron Capture ◽  
Neutron Capture Therapy ◽  
Tumor Bearing ◽  
Thermal Neutron Irradiation ◽  
Delivery Vehicles

Significant anti-tumor effects and longer survivals were observed in the tumor-bearing mice treated with spermidinium closo-dodecaborate-encapsulating liposomes after thermal neutron irradiation.

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