Boron neutron capture therapy for malignant melanoma: An experimental approach

Journal Article · Sat Jul 01 00:00:00 EDT 1989 · Pigment Cell Research; (USA)

DOI:https://doi.org/10.1111/j.1600-0749.1989.tb00220.x· OSTI ID:5225901

Larsson, B S; Larsson, B; Roberto, A ^[1]

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1. Uppsala Univ. (Sweden)

Previous studies have shown that some thioamides, e.g., thiouracil, are incorporated as false precursors into melanin during its synthesis. If boronated analogs of the thioamides share this property, the melanin of melanotic melanomas offers a possibility for specific tumoural uptake and retention of boron as a basis for neutron capture therapy. We report on the synthesis of boronated 1H-1,2,4-triazole-3-thiol (B-TZT), boronated 5-carboxy-2-thiouracil (B-CTU), and boronated 5-diethylaminomethyl-2-thiouracil (B-DEAMTU) and the localization of these substances in melanotic melanomas transplanted to mice. The distribution in the mice was studied by boron neutron capture radiography. B-TZT and B-CTU showed the highest tumour:normal tissue concentration ratios, with tumour:liver ratios of about 4 and tumour:muscle ratios of about 14; B-DEAMTU showed corresponding ratios of 1.4 and 5, respectively. The absolute concentration of boron in the tumours, however, was more than three times higher in the mice injected with B-TZT, compared with B-CTU. The results suggest that B-TZT may be the most promising compound of the three tested with regard to possible therapy of melanotic melanomas.

• OSTI ID: 5225901
• Journal Information: Pigment Cell Research; (USA), Journal Name: Pigment Cell Research; (USA) Vol. 2:4; ISSN 0893-5785; ISSN PCREE
• Country of Publication: United States
• Language: English

Related Subjects

550603* -- Medicine-- External Radiation in Therapy-- (1980-)
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
ANTIMETABOLITES
ANTITHYROID DRUGS
AZINES
BARYONS
BORON 10
BORON COMPOUNDS
BORON ISOTOPES
DISEASES
DISTRIBUTION
DRUGS
ELEMENTARY PARTICLES
EXPERIMENTAL NEOPLASMS
FERMIONS
HADRONS
HETEROCYCLIC COMPOUNDS
HORMONE ANTAGONISTS
HYDROXY COMPOUNDS
ISOTOPES
LIGHT NUCLEI
MAMMALS
MEDICINE
MELANOMAS
MICE
NEOPLASMS
NEUTRON CAPTURE THERAPY
NEUTRON THERAPY
NEUTRONS
NUCLEAR MEDICINE
NUCLEI
NUCLEONS
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC SULFUR COMPOUNDS
PYRIMIDINES
RADIOLOGY
RADIOTHERAPY
RODENTS
STABLE ISOTOPES
THERAPY
THIOLS
THIOURACIL
TISSUE DISTRIBUTION
UPTAKE
URACILS
VERTEBRATES