| 摘要 |
<p>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 should be useful to provide anti-gout and/or anti-neoplastic therapeutic agents or will serve as potentiators for other such agents. The most preferred, potent tight-binding multisubstrate adduct inhibitor of glycinamide ribonucleotide transformylase, is N10-[5'-phosphoribosyl-1'-β-aminocarbonylmethyl-1-thioacetyl]-5,8-dideazafolate, which has the chemical formula (I).</p> |
