Boron-containing thiouracil derivatives for neutron-capture therapy of melanoma.
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.
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Department of Chemistry, University of Bremen, Federal Republic of Germany.
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D000818:Animals; D001895:Boron / Q000627:therapeutic use*; D007202:Indicators and Reagents; D008546:Melanoma, Experimental / Q000532:radiotherapy*; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D009502:Neutrons; D013329:Structure-Activity Relationship; D013889:Thiouracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use
D007202:Indicators and Reagents; D013889:Thiouracil; D001895:Boron