[BOF-A1 and BOF-A2, new 5-FU degradation-inhibitory agents].
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.
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000627:therapeutic use; D005467:Floxuridine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000627:therapeutic use; D005472:Fluorouracil / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism* / Q000627:therapeutic use; D008099:Liver / Q000378:metabolism; D051379:Mice; D011725:Pyridines / Q000008:administration & dosage / Q000378:metabolism; D011743:Pyrimidines / Q000378:metabolism; D051381:Rats; D012510:Sarcoma 180 / Q000188:drug therapy; D012513:Sarcoma, Experimental / Q000188:drug therapy* / Q000378:metabolism; D012517:Sarcoma, Yoshida / Q000188:drug therapy; D005641:Tegafur / Q000008:administration & dosage; D014498:Uracil / Q000008:administration & dosage
D000970:Antineoplastic Agents; D011725:Pyridines; D011743:Pyrimidines; D005467:Floxuridine; C053193:BOF A1; D005641:Tegafur; C053195:2,6-dihydroxy-3-cyanopyridine; D014498:Uracil; C053194:Emitefur; C030986:pyrimidine; C023666:pyridine; D005472:Fluorouracil