Synthesis of 10-acetyl-5,8-dideazafolic acid: a potent inhibitor of glycinamide ribonucleotide transformylase.
10-Acetyl-5,8-dideazafolic acid has been synthesized in good yield from the parent compound, 5,8-dideazafolic acid. This quinazoline folate analogue showed no activity as a substrate for the folate-requiring de novo purine biosynthetic enzyme glycinamide ribonucleotide transformylase isolated from the murine lymphoma cell line L5178Y, but proved to be a potent competitive inhibitor, Ki = 1.3 microM, of the purified enzyme.
D000217:Acyltransferases / Q000037:antagonists & inhibitors*; D005492:Folic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D019877:Hydroxymethyl and Formyl Transferases; D007700:Kinetics; D051026:Phosphoribosylglycinamide Formyltransferase
D005492:Folic Acid; C050336:10-acetyl-5,8-dideazafolic acid; D019877:Hydroxymethyl and Formyl Transferases; D051026:Phosphoribosylglycinamide Formyltransferase; D000217:Acyltransferases