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Biological efficacy of a boronated imidocaptate for neutron capture

Conference · · Transactions of the American Nuclear Society; (United States)
OSTI ID:5864698
;  [1];  [2];
  1. Brookhaven National Lab., Upton, NY (United States)
  2. Karkinos Biochem, Inc., Chandler, AZ (United States)
Neutron capture therapy (NCT) is a binary system that utilizes intracellular {sup 10}B as a target atom for subsequent activation by thermal neutrons according to the {sup 10}B(n,{alpha}){sup 7}Li reaction. In the 1950s, clinical trials of NCT for the treatment of malignant brain tumors were unsuccessful because of (a) the poor penetration of the thermal neutrons and (b) the lack of boron compounds that would give high tumor-to-normal-tissue ratios. The recent development of epithermal neutron beams should permit greater neutron penetration to the depth of the tumor. Additionally, second- and third-generation boron compounds have been synthesized. Many of these are being investigated for their potential use in NCT. Among these are nitroimidazoles. Nitroimidazoles have been of interest as photon radiation sensitizers and have the characteristics of facile tumor penetration and susceptibility to nitroreduction in the tumor. This latter characteristic yields metabolites that bind to cellular macromolecules. Such binding may interfere with DNA repair, and this may be a mechanism in the synergizing activity of the nitroimidazole for alkylating agents or hyperthermia. The DNA repair inhibition, in addition to oxygen enhancement, may play a role in the observed ability of nitroimidazoles to synergize the photon therapy of tumors. The authors took advantage of these features to use this class of compounds as a carrier of boron for NCT.
OSTI ID:
5864698
Report Number(s):
CONF-910603--
Conference Information:
Journal Name: Transactions of the American Nuclear Society; (United States) Journal Volume: 63
Country of Publication:
United States
Language:
English

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