Boron-containing thiouracil derivatives for neutron-capture therapy of melanoma

Journal Article · Tue Jan 01 04:00:00 EST 1991 · Journal of Medicinal Chemistry; (USA)

DOI:https://doi.org/10.1021/jm00105a049· OSTI ID:6054873

Tjarks, W; Gabel, D ^[1]

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1. Univ. of Bremen (Germany, F.R.)

Boron-containing derivatives of 2-thiouracil and 2,4-dithiouracil and the corresponding 6-propyl compounds, containing a dihydroxyboryl group in the 5-position, have been prepared. These compounds accumulate in B16 melanoma in mice in concentrations up to 30 micrograms of boron per gram tissue. The uptake persists. The toxicity of both 2-thiouracil derivatives is low. These compounds are therefore good candidates for boron neutron-capture therapy of malignant melanoma.

• OSTI ID: 6054873
• Journal Information: Journal of Medicinal Chemistry; (USA), Journal Name: Journal of Medicinal Chemistry; (USA) Vol. 34:1; ISSN JMCMA; ISSN 0022-2623
• Country of Publication: United States
• Language: English

Related Subjects

550603* -- Medicine-- External Radiation in Therapy-- (1980-)
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BORON COMPOUNDS
CHEMICAL PREPARATION
DISEASES
DRUGS
EXPERIMENTAL NEOPLASMS
LABELLED COMPOUNDS
MAMMALS
MEDICINE
MELANOMAS
MICE
NEOPLASMS
NEUTRON CAPTURE THERAPY
NEUTRON THERAPY
NUCLEAR MEDICINE
RADIOLOGY
RADIOPHARMACEUTICALS
RADIOTHERAPY
RODENTS
STRUCTURE-ACTIVITY RELATIONSHIPS
SYNTHESIS
THERAPY
VERTEBRATES