Abstract
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.
Publication types
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Acyltransferases / antagonists & inhibitors*
-
Folic Acid / analogs & derivatives*
-
Folic Acid / chemical synthesis
-
Folic Acid / pharmacology
-
Hydroxymethyl and Formyl Transferases*
-
Kinetics
-
Phosphoribosylglycinamide Formyltransferase
Substances
-
Folic Acid
-
10-acetyl-5,8-dideazafolic acid
-
Hydroxymethyl and Formyl Transferases
-
Phosphoribosylglycinamide Formyltransferase
-
Acyltransferases