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FLUORINATED PYRIMIDINES. XXIV. IN VIVO METABOLISM OF 5-TRIFLUOROMETHYLURACIL-2-C-14 AND 5-TRIFLUOROMETHYL-2'-DEOXYURIDINE-2-C-14.

作者:Charles Heidelberger, Judith Boohar, Bernard H. Kampschroer · 发表于:PubMed · 年份:1965 · 被引用次数:45 · 研究领域:Biochemical and Molecular Research、Cancer, Hypoxia, and Metabolism、Colorectal Cancer Treatments and Studies

Summary The excretion, distribution, and metabolism in tumor bearing mice of 5-trifluoromethyluracil-2-C14, 5-trifluoromethyl-2′-deoxyuridine-2-C14, and 5-carboxyuracil-2-C14 have been studied. In contrast to all other pyrimidines, the ring of these compounds is not metabolically degraded. The nucleoside is cleaved to the pyrimidine base, and 5-carboxyuracil is the only catabolite formed. The tissue distribution of radioactivity has been determined, and there is no selective localization in the tumor. 5-Trifluoromethyl-2′-deoxyuridine is incorporated into the deoxyribonucleic acid (DNA) of these tissues, but to a very small extent. The deoxyribonucleoside mono-, di-, and triphosphates have been demonstrated as anabolic products in the tissues. In the tissues studied the catabolism is least in the tumor and most in the intestines.