Boron-containing nucleosides for neutron capture therapy
There is widespread and increasing interest in the preparation of organoboron compounds for their potential medical application for neutron capture therapy (NCT). The authors approach was to synthesize a boron-containing pyrimidine nucleoside,5-dihydroxyboryl-2'-deoxyuridine (DBDU), which could act as a sensitizing agent in boron neutron-capture reactions. Irradiation of tumor cells that have incorporated boron nucleoside with neutrons would, therefore, principally destroy only tumor tissue. Since the nucleoside would be localized primarily in the nucleus, the greater biological efficacy would permit utilization of lower boron concentrations. Synthetic procedures to novel boron nucleosides and pyrimidines that could be of potential utility for NCT have been worked out. These include the synthesis of 2-thio-5-dihydroxyboryluracil and 2,4-dithio-5-dihydroxyboryluracil, which may be taken up selectively in melanoma cells as analogues of 2-thiouracil; and 6-dihydroxyborylpurine-2'-deoxyriboside, an analogue of 2'-deoxyadenosine. Studies with these compounds will allow the authors to determine the potential use of these boron nucleosides and pyrimidines for boron NCT, with the aim of reducing mortality and increasing life span of patients with diagnosed gliomas, melanomas and other tumors.
- Research Organization:
- VA Medical Center, Atlanta, GA
- OSTI ID:
- 6718122
- Report Number(s):
- CONF-861102-
- Journal Information:
- Trans. Am. Nucl. Soc.; (United States), Vol. 53; Conference: American Nuclear Society and Atomic Industrial Forum joint meeting, Washington, DC, USA, 16 Nov 1986
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
NEOPLASMS
NEUTRON CAPTURE THERAPY
NUCLEOSIDES
BORON 10
GLIOMAS
IRRADIATION
NUCLEAR MEDICINE
PYRIMIDINES
SOLUBILITY
UPTAKE
AZINES
BORON ISOTOPES
DISEASES
HETEROCYCLIC COMPOUNDS
ISOTOPES
LIGHT NUCLEI
MEDICINE
NEUTRON THERAPY
NUCLEI
NUCLEOTIDES
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
RADIOLOGY
RADIOTHERAPY
RIBOSIDES
STABLE ISOTOPES
THERAPY
550603* - Medicine- External Radiation in Therapy- (1980-)