[Studies of the antitumor activity and enzymology of 2'-deoxy-5-fluorouridine (FdUrd) derivatives].
The antitumor activity and enzymology of 2'-deoxy-3', 5'-bis-O-(4-methoxyphenoxycarbonyl)-5-fluoro-3-(4-n-Propoxybenz oyl uridine (FF-707) were examined. It was found that stability in small intestine homogenate of FF-707 was higher than that of FF-705 [2'-deoxy-3', 5'-O-diacetyl-5-fluoro-3-(3 methylbenzoyl) uridine]. Reduction of the tumor weight was greater in mice bearing sarcoma-180 and rats bearing Yoshida sarcoma treated with the oral administration of FF-707 than that FF-705. The relationship between the antitumor activity and the inhibition of thymidylate synthase after the oral administration of FF-707 was examined. The extent of the inhibition of thymidylate synthase seemed to be parallel to that of the inhibition of the tumor growth.
D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism / Q000494:pharmacology*; D005467:Floxuridine / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D007421:Intestine, Small / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D012510:Sarcoma 180 / Q000473:pathology; D012513:Sarcoma, Experimental / Q000201:enzymology / Q000473:pathology*; D012517:Sarcoma, Yoshida / Q000473:pathology; D013940:Thymidylate Synthase / Q000037:antagonists & inhibitors
D000970:Antineoplastic Agents; D005467:Floxuridine; C040250:2'-deoxy-3',5'-di-O-acetyl-5-fluoro-3-(3-methylbenzoyl)uridine; D013940:Thymidylate Synthase