Gar transformylase inhibitor

Details Gar transformylase inhibitor Gar transformylase inhibitor

C - Chemistry, Metallurgy

07

H

167/202, 260/229

C07H 5/04 (2006.01) A61K 31/70 (2006.01) C07H 11/04 (2006.01) C07H 13/04 (2006.01)

Patent

CA 2002765

Docket No. 38,243 GAR TRANSFORMYLASE INHIBITOR ABSTRACT OF THE DISCLOSURE The present invention is directed to several multisubstrate adduct inhibitors of glycinamide ribonucleotidew 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 preferred, potent tight-binding multisubstrate adduct inhibitor of glycinamide ribonucleotide transformylase, is N10-[5'-phosphoribosyl-1'-.beta.-aminocarbonylmethyl- 1-thioacatyl]-5,8-dideazafolate, which has the chemical formula: Image .beta.-TGDDF

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