Synthesis of quinazoline analogs of isofolic acid.
Four quinazoline analogs of isofolic acid were synthesized including 5-methyl-5,8-deazaisofolic acid (8a), 5,8-deazaisofolic acid (8c), as well as their 4-NH2 counterparts 8b and 8d. None of these showed significant activity against L1210 leukemia in mice at dose levels where amethopterin provided significant prolongation in survival.
D000818:Animals; D005492:Folic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use; D005493:Folic Acid Antagonists; D066298:In Vitro Techniques; D007939:Leukemia L1210 / Q000188:drug therapy; D008099:Liver / Q000201:enzymology; D051379:Mice; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D013329:Structure-Activity Relationship
D005493:Folic Acid Antagonists; D011799:Quinazolines; D005492:Folic Acid