GAR transformylase inhibitor

摘要

The present invention is directed to several multisubstrate adduct inhibitors of glycinamide ribonucleotide transformylase (GAR TFase; E.C. 2.1.2.2), a folate-requiring enzyme of de novo purine biosynthesis. The compounds of the present invention will be useful to provide anti-gout and/or anti-neoplastic therapeutic agents or will serve as potentiators for other such agents. The most prefeffed, potent tight-binding multisubstrate adduct inhibitor of glycinamide ribonucleotide transformylase, is N10-[5'-phosphoribosyl-1'- beta -aminocarbonylmethyl-1-thioacetyl]-5,8-dideazafolate, which has the chemical formula: <IMAGE>