Abstract
2, 6-Dihydroxy-3-cyano pyridine (CNDP) was found from the study of inhibitory effects of pyrimidine and pyridine derivatives on 5-FU degradation catalyzed by dihydrouracil dehydrogenase. CNDP, a new inhibitor on 5-FU degradation was 300 times more effective than uracil. Co-administration of an equi-molar CNDP with some fluorinated pyrimidine preparations potentiated their antitumor activity. Tegafur (FT-207) and EM-FU in combination with CNDP were found most effective. This potentiation was exhibited not only to 5-FU derivatives but also to FdUrd and its derivatives. BOF-A1 and BOF-A2, new compounds combined with CNDP were markedly active against mouse sarcoma 180 and rat Yoshida sarcoma.
MeSH terms
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Animals
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Antineoplastic Agents / therapeutic use*
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Antineoplastic Combined Chemotherapy Protocols / therapeutic use
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Floxuridine / administration & dosage
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Floxuridine / analogs & derivatives*
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Floxuridine / therapeutic use
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Fluorouracil / administration & dosage
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Fluorouracil / analogs & derivatives*
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Fluorouracil / metabolism*
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Fluorouracil / therapeutic use
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Liver / metabolism
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Mice
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Pyridines / administration & dosage
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Pyridines / metabolism
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Pyrimidines / metabolism
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Rats
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Sarcoma 180 / drug therapy
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Sarcoma, Experimental / drug therapy*
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Sarcoma, Experimental / metabolism
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Sarcoma, Yoshida / drug therapy
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Tegafur / administration & dosage
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Uracil / administration & dosage
Substances
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Antineoplastic Agents
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Pyridines
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Pyrimidines
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Floxuridine
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BOF A1
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Tegafur
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2,6-dihydroxy-3-cyanopyridine
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Uracil
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Emitefur
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pyrimidine
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pyridine
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Fluorouracil